盐酸司来吉兰 | 14611-52-0

• 物质功能分类: 原料药 - 消化系统用药 - 食欲抑制药及其它减肥药
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 盐酸司来吉兰
• 中文别名: 盐酸丙炔苯并胺；(R)-N,alpha-二甲基-N-(2-丙炔基)苯乙胺盐酸盐；盐酸司立吉林
• 英文名称: (R)-(-)-deprenyl hydrochloride
• 英文别名: selegiline hydrochloride；L-deprenyl hydrochloride；hydron;(2R)-N-methyl-1-phenyl-N-prop-2-ynylpropan-2-amine;chloride
• CAS: 14611-52-0
• 化学式: C₁₃H₁₇N*ClH
• 分子量: 223.746
• InChiKey: IYETZZCWLLUHIJ-UTONKHPSSA-N

物化性质

• 熔点：
  141-142°C
• 比旋光度：
  D25 -10.8° (c = 6.48 in water)
• 溶解度：
  H2O: >10 mg/mL
• 颜色/状态：
  Crystals
• 碰撞截面：
  141 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  3.2
• 氢给体数：
  1
• 氢受体数：
  1

ADMET

代谢

塞来吉林主要通过尿液以结合型和未结合型代谢物形式排出。口服给药的塞来吉林剂量中约有20-63%以l-甲基安非他明形式、9-26%以l-安非他明形式、1%以l-去甲基塞来吉林形式在尿液中排出。

Selegiline is excreted principally in urine as conjugated and unconjugated metabolites. About 20-63% of an orally administered dose of selegiline is excreted in urine as l-methamphetamine, 9-26% as l-amphetamine, and 1% as l-demethylselegiline. /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

代谢

迅速且完全代谢为N-去甲基金思卡林、l-甲基苯丙胺和l-苯丙胺。

Rapidly and completely metabolized to N-desmethyldeprenyl, l-methamphetamine, and l-amphetamine.

来源:Hazardous Substances Data Bank (HSDB)

代谢

塞来吉林被广泛代谢，可能是通过细胞色素P450介导的氧化作用，形成L-去甲塞来吉林和L-甲基安非他明，后者进一步代谢为L-安非他明。塞来吉林在肺中也代谢为L-去甲塞来吉林和L-甲基安非他明，在肾脏中代谢为L-甲基安非他明，但与肝脏相比，这些组织中代谢的程度是微不足道的。/塞来吉林/

Selegiline is extensively metabolized, presumably through cytochrome p450 mediated oxygenation, to form l-desmethylselegiline and l-methamphetamine, which is further metabolized to l-amphetamine. Selegiline also is metabolized in the lungs to l-desmethylselegiline and l-methamphetamine and in the kidneys to l-methamphetamine, but the degree of metabolism in these tissues is minimal compared with that in the liver. /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

代谢

... 塞利吉林的药代动力学具有高度变异性。口服10毫克塞利吉林后，它会被迅速吸收并代谢为去甲基塞利吉林、左旋安非他明和左旋甲基安非他明。/塞利吉林/

... The pharmacokinetics of selegiline are highly variable. Following an oral dose of selegiline 10 mg, it is rapidly absorbed and metabolized to desmethylselegiline, levoamphetamine and levomethamphetamine. /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：据报道，在母乳喂养期间使用司来吉兰的临床经验非常有限。尽管在哺乳婴儿中没有报告不良反应，但可能更倾向于使用其他药物，特别是在哺乳新生儿或早产儿时。司来吉兰透皮贴剂的制造商建议在治疗期间和最后一剂后7天内不推荐哺乳。 ◉ 对哺乳婴儿的影响：一名妇女在怀孕期间每天服用司来吉兰10毫克、左旋多巴400毫克和苯丝拉齐100毫克，并在哺乳婴儿3天期间继续服用。孩子被随访了10年，没有发现发育异常。 一名患有严重抑郁症的妇女在怀孕和产后期间每天使用6毫克司来吉兰贴剂。她专门哺乳婴儿一段时间。在婴儿5个月大时进行的儿科随访发现，婴儿发育正常。 ◉ 对泌乳和母乳的影响：司来吉兰可以降低患有偏头痛的女性以及那些服用神经阻滞药物的女性的血清催乳素水平。这些发现对哺乳母亲的临床相关性尚不清楚。在已建立泌乳的母亲中，催乳素水平可能不会影响她的哺乳能力。

◉ Summary of Use during Lactation:A minimal amount of clinical use of selegiline during breastfeeding has been reported. Although no adverse reactions have been reported in the breastfed infants, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. The manufacturer of the selegiline transdermal patch recommends that breastfeeding is not recommended during treatment and for 7 days after the final dose. ◉ Effects in Breastfed Infants:A woman took selegiline 10 mg, levodopa 400 mg and benserazide 100 mg daily throughout pregnancy and continued them while breastfeeding her infant for 3 days. The child was followed for 10 years and no developmental abnormalities were found. A woman with severe depression used a selegiline patch 6 mg per day during pregnancy and postpartum. She exclusively breastfed her infant for an unstated period of time. Pediatric follow-up at 5 months of age found that the infant was developing normally. ◉ Effects on Lactation and Breastmilk:Selegiline can decrease serum prolactin in women with migraine, and in those taking neuroleptic drugs. The clinical relevance of these findings in nursing mothers is not known. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

来源:Drugs and Lactation Database (LactMed)

毒理性

• 相互作用

尽管一些病人在接受非选择性单胺氧化酶抑制剂治疗期间对拟交感神经药物的高血压作用似乎较为敏感，但是通常可以将含有升压剂（例如，麻黄碱、苯丙醇胺）的非处方（柜台销售，OTC）或处方感冒或干草热制剂给予每日接受10毫克或更少剂量司来吉兰盐酸的患者，而不至于有过度的未控制高血压的风险。然而，至少有一名患者在接受推荐的每日10毫克司来吉兰盐酸和一种拟交感神经药物（麻黄碱）治疗时发生了高血压危机。

Although some patients appear to be sensitive to the hypertensive effects of sympathomimetic agents during therapy with a nonselective MAO inhibitor, nonprescription (over-the-counter, OTC) or prescription cold or hay fever preparations that contain pressor agents (e.g., ephedrine, phenylpropanolamine) generally can be given to patients receiving selegiline hydrochloride dosages of 10 mg or less daily without undue risk of uncontrolled hypertension. However, hypertensive crisis was reported in at least one patient receiving the recommended 10 mg daily dosage of selegiline hydrochloride and a sympathomimetic agent (ephedrine).

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

在接受左旋多巴治疗的病人中，添加盐酸司来吉兰可能会加剧与左旋多巴相关的运动障碍。这种效应在临床试验中接受该药物治疗的平均28%（范围：4-90%）的病人中出现，通常在开始司来吉兰治疗后的2周内发生，并且通常在减少左旋多巴剂量时得到缓解……。在接受左旋多巴和每日超过10毫克盐酸司来吉兰治疗的病人中，已经出现了磨牙、肌肉抽搐和肌阵挛性抽动。

In patients receiving levodopa, addition of selegiline hydrochloride may exacerbate levodopa-associated dyskinesias. This effect, which occurred in an average of 28% (range: 4-90%) of patients receiving the drug in clinical trials, usually occurs within 2 weeks after initiating selegiline therapy and generally is mitigated when the levodopa dosage is reduced ... . Bruxism, muscle twitching and myoclonic jerks have occurred in patients receiving levodopa and selegiline hydrochloride dosages exceeding 10 mg daily.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

心脏停搏、出汗、高血压、晕厥、行为和精神状态改变、意识障碍、高热、癫痫、肌肉强直和颤抖在使用司来吉兰和三环类抗抑郁药时已有发生。不推荐同时使用；在停用司来吉兰和开始使用三环类抗抑郁药之间至少应间隔14天。/司来吉兰/

Asystole, diaphoresis, hypertension, syncope, changes in behavior and mental status, impaired consciousness, hyperpyrexia, seizures, muscular rigidly, and tremors have occurred with concurrent use of selegiline and tricyclic antidepressants. Concurrent use is not recommended; at least 14 days should elapse between discontinuation of selegiline and initiation of a tricyclic antidepressant. /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

极少数情况下，在同时使用选择性血清素再摄取抑制剂（SSRIs）和司来吉兰后，报告了一种类似血清素综合症的反应。（血清素综合症可能是由于将一个血清素能药物与单胺氧化酶抑制剂结合使用而发生的。这种综合症可能表现为精神状态改变[混淆、轻躁症]、不安、肌阵挛、反射亢进、出汗、寒战、震颤、腹泻、不协调和/或发热。如果早期发现，通常在撤除引起问题的药物后综合症会迅速解决。）由于存在自主神经系统不稳定、肌肉僵硬、严重激越或谵妄的风险，不建议同时使用司来吉兰和SSRIs。在停止使用单胺氧化酶抑制剂和开始使用SSRI之间，至少应间隔14天。然而，由于氟西汀及其活性代谢物半衰期较长，在停止使用氟西汀和开始使用单胺氧化酶抑制剂之间，至少应间隔5周（大约5个半衰期）。另外，根据文拉法辛的半衰期，在停止使用文拉法辛和开始使用单胺氧化酶抑制剂之间，至少应间隔7天。/司来吉兰/

A reaction resembling the serotonin syndrome has been reported rarely following concurrent use of selegiline with selective serotonin re-uptake inhibitors (SSRIs). (The serotonin syndrome may occur as the result of combining a serotonergic agent with an MAO inhibitor. The syndrome may be manifest by mental status changes (confusion, hypomania), restlessness, myoclonus, hyperreflexia, diaphoresis, shivering, tremor, diarrhea, incoordination, and/or fever. If recognized early, the syndrome usually resolves quickly upon withdrawal of the offending agents.) Concurrent use of selegiline with SSRIs is not recommended because of the potential for autonomic instability, muscular rigidity, severe agitation, or delirium. At least 14 days should elapse between discontinuation of an MAO inhibitor and initiation of an SSRI. However, because of the long half-lives of fluoxetine and its active metabolite, at least 5 weeks (approximately 5 half-lives) should elapse between discontinuation of fluoxetine and initiation of therapy with an MAO inhibitor. ALso, based on the half-life of venlafaxine, at least 7 days should elapse between discontinuation of venlafaxine and initiation of therapy with an MAO inhibitor. /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

塞来吉林及其代谢物在体内广泛分布，并能穿过血脑屏障。在给小鼠静脉注射放射性标记的盐酸塞来吉林后，母药和/或代谢物会迅速广泛地分布到大脑、肝脏、肾脏、肺、心脏和棕色脂肪中。在健康成年人静脉注射放射性标记的盐酸塞来吉林后，放射性物质在丘脑、基底神经节、中脑和扣带皮层中累积最多。

Selegiline and its metabolites are widely distributed into body tissues and cross the blood-brain barrier. Following IV administration of radiolabeled selegiline hydrochloride in mice, the parent drug and/or metabolites are rapidly and widely distributed to brain, liver, kidney, lung, heart, and brown fat. Following IV administration of radiolabeled selegiline hydrochloride in healthy adults, the highest accumulation of radioactivity occurred in the thalamus, basal ganglia, mesencephalon, and cingulate gyrus. /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

塞来吉林主要通过尿液以结合型和未结合型代谢物形式排出。口服给药的塞来吉林的大约20-63%以l-甲基苯丙胺的形式在尿液中排出，9-26%以l-苯丙胺的形式排出，1%以l-去甲基塞来吉林的形式排出。...在大约72小时内，大约15%的剂量以粪便形式排出。/SRP：如果没有对样本进行d/l-异构体鉴定，这通常会导致对d-甲基苯丙胺的误检阳性结果。/ /塞来吉林/

Selegiline is excreted principally in urine as conjugated and unconjugated metabolites. About 20-63% of an orally administered dose of selegiline is excreted in urine as l-methamphetamine, 9-26% as l-amphetamine, and 1% as l-demethylselegiline. ... About 15% of a dose is excreted in feces within 72 hours following administration of selegiline. /SRP: This would usually result in a false positive drug test for d-methamphetamine if no d/l-isomer characterization was performed on the specimen./ /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

从胃肠道迅速吸收。

Rapidly absorbed from the gastrointestinal tract.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

... 平均血浆峰浓度（Cmax）约为2微克/升，达到峰值的时间在一小时之内。塞来昔布的绝对生物利用度大约为10%。它具有1854升的表观分布容积。塞来昔布的口服清除率（59升/分钟）远高于肝脏血流量（1.5升/分钟），这表明塞来昔布的消除过程中涉及到了肝外过程。... /塞来昔布/

... The mean peak plasma concentration (Cmax) is approximately 2 ug/L and the time to reach the peak is under an hour. The absolute bioavailability of selegiline is approximately 10%. It has an apparent volume of distribution of 1854 L. The oral clearance of selegiline (59 L/min) is many fold higher than the liver blood flow (1.5 L/min), indicating that extrahepatic processes are involved in the elimination of selegiline. ... /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

... Selegiline 从胃肠道被快速吸收，并且口服给药后迅速进入大脑和脊髓。该药物与大脑中含有高水平MAO-B的区域结合，例如丘脑、纹状体、大脑皮层和脑干。... /司来吉兰/

... Selegiline is readily absorbed from the gastrointestinal tract and rapidly enters the brain and spinal cord following oral administration. The drug binds to brain regions with a high MAO-B content, such as the thalamus, the striatum, the cortex, and the brainstem. ... /Selegiline/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  6.1(b)
• 安全说明：
  S22,S26
• WGK Germany：
  3
• 海关编码：
  2921519090
• 危险品运输编号：
  UN 3249
• RTECS号：
  DA0292500
• 包装等级：
  III
• 危险类别：
  6.1(b)
• 储存条件：
  存储于室温下

SDS

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Section 1. Chemical Product and Company Identification
Selegiline Hydrochloride
Common Name/
Trade Name
Manufacturer
Commercial Name(s)
Synonym
Chemical Name
Chemical Family
Selegiline Hydrochloride

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Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water
for at least 15 minutes. Cold water may be used. Get medical attention.
Skin Contact In case of contact, immediately flush skin with plenty of water. Cover the irritated skin with an emollient.
Remove contaminated clothing and shoes. Cold water may be used.Wash clothing before reuse.
Thoroughly clean shoes before reuse. Get medical attention.
Serious Skin Contact Wash with a disinfectant soap and cover the contaminated skin with an anti-bacterial cream. Seek
immediate medical attention.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen.
Get medical attention.
Serious Inhalation Not available.
Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to
an unconscious person. If large quantities of this material are swallowed, call a physician immediately.
Loosen tight clothing such as a collar, tie, belt or waistband.
Serious Ingestion Not available.

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Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Not available.
Flash Points
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...).
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances Non-flammable in presence of shocks.
Risks of explosion of the product in presence of mechanical impact: Not available.
Explosion Hazards in
Risks of explosion of the product in presence of static discharge: Not available.
Presence of Various
Substances
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on Not available.
Fire Hazards
Special Remarks on Explosion Not available.
Hazards

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Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by
spreading water on the contaminated surface and dispose of according to local and regional authority
requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading
water on the contaminated surface and allow to evacuate through the sanitary system.
Selegiline Hydrochloride

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Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Empty containers pose a fire risk, evaporate the
residue under a fume hood. Ground all equipment containing material. Do not ingest. Do not breathe dust.
Wear suitable protective clothing. In case of insufficient ventilation, wear suitable respiratory equipment. If
ingested, seek medical advice immediately and show the container or the label. Avoid contact with skin and
eyes.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area.

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Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels
below recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep
exposure to airborne contaminants below the exposure limit.
Personal Protection Splash goggles. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent.
Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be
a Large Spill used to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a
specialist BEFORE handling this product.
Exposure Limits Not available.

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Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (Crystalline powde) Odor Not available.
Not available.
Taste
223.75 g/mole
Molecular Weight
Color White.
pH (1% soln/water) Not available.
Boiling Point Not available.
Melting Point 141°C (285.8°F) - 145 C.
Not available.
Critical Temperature
Specific Gravity Not available.
Not applicable.
Vapor Pressure
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Not available.
Ionicity (in Water)
Dispersion Properties See solubility in water.
Soluble in cold water, hot water.
Solubility

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Section 10. Stability and Reactivity Data
The product is stable.
Stability
Instability Temperature Not available.
Excess heat
Conditions of Instability
Incompatibility with various Not available.
substances
Corrosivity Not available.
Selegiline Hydrochloride
Sensitive to light.
Special Remarks on
Reactivity
Not available.
Special Remarks on
Corrosivity
Polymerization Will not occur.

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Section 11. Toxicological Information
Routes of Entry Inhalation. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 385 mg/kg [Rat].
Chronic Effects on Humans Not available.
Other Toxic Effects on Hazardous in case of ingestion.
Humans Slightly hazardous in case of skin contact (irritant), of inhalation.
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on May cause adverse reproductive effects and birth defects (teratogenic) based on animal test data
Chronic Effects on Humans
Special Remarks on other Acute Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation.
Eyes: May cause eye irritation.
Inhalation: May cause respiratory tract irritation.
Ingestion: Harmful if swallowed. May cause gastrointestinal tract irritation with nausea, high fever, inability
to keep mouth open (trismus), hyperextension and spasticity, increased or profuse sweating (diaphoresis).
May affect behavior/Cental Nervous System (agitation, anxiety, hallucinations, drowsiness, dizziness,
faintness, irritability, hyperactivity, confusion), cardiovascular system (hypotension, hypertension, irregular
pulse, rapid pulse, vascular collapse, seizures, coma), respiration (respiratory depression or failure).
It is metobolized to Methylamphetamine and Amphetamine (-) isomers.
Conditions aggravated by exposure: Allergic reaction to amphetamine, ephedrine, etc., pregnancy,
glaucoma, over active thyroid, severe anxiety.

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Section 12. Ecological Information
Ecotoxicity Not available.
BOD5 and COD Not available.
Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation
products may arise.
Toxicity of the Products The products of degradation are less toxic than the product itself.
of Biodegradation
Not available.
Special Remarks on the
Products of Biodegradation

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Section 13. Disposal Considerations
Waste must be disposed of in accordance with federal, state and local environmental
Waste Disposal
control regulations.

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Not applicable.
Identification
Special Provisions for Not applicable.
Transport
Selegiline Hydrochloride
DOT (Pictograms)

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Section 15. Other Regulatory Information and Pictograms
No products were found.
Federal and State
Regulations
California prop. 65: This product contains the following ingredients for which the State of California has
California
found to cause cancer which would require a warning under the statute: No products were found.
Proposition 65
Warnings
California prop. 65: This product contains the following ingredients for which the State of California has
found to cause birth defects which would require a warning under the statute: No products were found.
Other Regulations OSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200).
WHMIS (Canada) CLASS D-1B: Material causing immediate and serious toxic effects (TOXIC).
Other Classifications
DSCL (EEC) R22- Harmful if swallowed. S46- If swallowed, seek medical advice
immediately and show this container or label.
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.
Selegiline Hydrochloride

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

简介

盐酸司来吉兰片是一种选择性单胺氧化酶B（MAO-B）不可逆抑制剂，主要作用是阻断多巴胺的代谢，从而延长多巴胺的作用时间。它还能抑制突触多巴胺的再摄取。

应用

盐酸司来吉兰片适用于治疗帕金森病，常作为左旋多巴和美多巴等药物的辅助用药。

反应信息

• 作为反应物：
  描述：

  盐酸司来吉兰 在 sodium carbonate 作用下， 反应 1.0h， 以100%的产率得到司来吉兰 盐酸盐
  参考文献：
  名称：

  司来吉兰官能化的聚乙二醇化聚氰基丙烯酸烷基酯纳米颗粒：与淀粉样β肽相互作用和表面重组的研究

  摘要：

  阿尔茨海默氏病（AD）是一种神经退行性疾病，对于新疗法的研究极具挑战性。由于淀粉样β-肽1-42（Aβ（1-42））肽的原纤维形成被认为是神经元变性的主要原因，因此，针对该肽的芳香族分子已经引起了人们的特别关注。本文报道了司来吉林功能化和荧光聚氰基丙烯酸烷基酯纳米颗粒（NPs）的合成及其对Aβ（1-42）肽的靶向性的评估。合成策略依赖于两亲共聚物的设计，方法是先串联Knoevenagel-Michael加入氰基乙酸酯衍生物，然后使其在水溶液中自组装，得到相应的NP。使用了不同的氰基乙酸盐：（i）氰基乙酸十六烷基酯（HDCA）形成NP的疏水核; （ii）罗丹明B氰基乙酸盐（RCA），用于荧光；（iii）具有隐身特性的甲氧基聚（乙二醇）氰基乙酸酯（MePEGCA）和（iv）司来吉兰-聚（乙二醇）氰基乙酸酯（SelPEGCA），以获得所需的功能性。合成了两种不同的两亲共聚物，一种含司来吉兰的共聚

  DOI：

  10.1016/j.ijpharm.2011.01.015
• 作为产物：
  描述：

  司来吉兰 盐酸盐 在 盐酸 作用下， 以 异丙醇 为溶剂， 反应 2.0h， 以145 g的产率得到盐酸司来吉兰
  参考文献：
  名称：

  一种盐酸司来吉兰的合成工艺

  摘要：

  本发明涉及化学制药领域，具体涉及盐酸司来吉兰的制备方法。本发明方法避免了使用麻黄碱、伪麻黄碱、脱氧麻黄碱等管控品；本发明的原料廉价易得、合成路线短、生产安全环保、降低了合成成本。使用本发明制备方法，可以高收率得到高纯度的目标化合物，易于工业化的大规模生产。

  公开号：

  CN110668951B

文献信息

• 4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
  申请人：Dunn Robert

  公开号：US20080318941A1

  公开（公告）日：2008-12-25

  The present disclosure provides compounds having affinity for the 5-HT 6 receptor which are of the formula (I): wherein R 1 , R 2 , R 5 , R 6 , B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

  本公开提供了具有亲和力的化合物，其对5-HT 6 受体具有亲和力，其化学式为（I）： 其中R1、R2、R5、R6、B、D、E、G、Q、x和n如本文所定义。本公开还涉及制备这种化合物的方法、含有这种化合物的组合物以及使用这些化合物的方法。
• HETEROBICYCLIC COMPOUNDS
  申请人：Amgen Inc.

  公开号：US20130225552A1

  公开（公告）日：2013-08-29

  Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.

  Formula (I)的杂环化合物： 或其药用可接受的盐、互变异构体或立体异构体，如规范中所定义，并含有它们的组合物，以及制备这种化合物的方法。本文还提供了通过抑制PDE10来治疗由此可治疗的疾病或疾病的方法，如肥胖症、非胰岛素依赖型糖尿病、精神分裂症、躁郁症、强迫症、亨廷顿病等。
• Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
  申请人：D'Sidocky Neil R.

  公开号：US20080242694A1

  公开（公告）日：2008-10-02

  Provided herein are Heterocyclic Compounds having the following structure: wherein R 1 , R 2 , X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.

  本文提供具有以下结构的杂环化合物： 其中R1、R2、X、Y和Z如本文所定义，包含有效量杂环化合物的组合物，以及治疗或预防癌症、炎症性疾病、免疫疾病、代谢性疾病以及通过给予患者需要的有效量杂环化合物来抑制激酶途径治疗或预防的疾病的方法。
• Novel Bicyclic Pyridinones
  申请人：Pettersson Martin Youngjin

  公开号：US20120252758A1

  公开（公告）日：2012-10-04

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  所述化合物及其药用可接受的盐被披露，其中所述化合物具有如本文所定义的Formula I的结构。相应的药物组合物、治疗方法、合成方法和中间体也被披露。
• Isoindole-imide compounds and compositions comprising and methods of using the same
  申请人：Muller W. George

  公开号：US20070049618A1

  公开（公告）日：2007-03-01

  This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

  这项发明涉及异吲哚-亚胺化合物，以及它们的药物可接受的盐、溶剂化物、对映异构体和前药。这些化合物的使用方法和药物组合物已经公开。