非诺贝特酸 | 42017-89-0

• 物质功能分类: 分析化学 - 分析试剂 - 离子色谱试剂
• 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: 非诺贝特酸
• 中文别名: 2-[4-(氯苯甲酰基)苯氧基]-2-甲基丙酸；2-[4-(4-氯苯甲酰基)苯氧基]-2-甲基丙酸；非诺贝酸；2-(4-(4-氯苯甲酰)苯氧基)-2-甲基丙酸
• 英文名称: fenofibric acid
• 英文别名: 2-(4-(4-chlorobenzoyl)phenoxy)-2-methylpropanoic acid；2-[4-(4-chlorobenzoyl)-phenoxy]-2-methylpropionic acid；2-methyl-2-(4-(4-chlorobenzoyl)phenoxy)propionic acid；2-methyl-2-(4-(4-chlorobenzoyl)phenoxy)propanoic acid；2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoic acid
• CAS: 42017-89-0
• 化学式: C₁₇H₁₅ClO₄
• 分子量: 318.757
• InChiKey: MQOBSOSZFYZQOK-UHFFFAOYSA-N

物化性质

• 熔点：
  177-179°C
• 沸点：
  486.5±35.0 °C(Predicted)
• 密度：
  1.286±0.06 g/cm3(Predicted)
• 溶解度：
  可溶于氯仿（少许）、甲醇（少许）
• 碰撞截面：
  185.72 Ų [M-H]-; 177.78 Ų [M+H]+

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  63.6
• 氢给体数：
  1
• 氢受体数：
  4

ADMET

代谢

体外和体内代谢研究表明，非诺贝酸不会通过细胞色素P450同工酶发生显著氧化代谢。CYP1A2、CYP2A6、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6、CYP2E1和CYP3A4酶在非诺贝酸的代谢中不起作用。相反，非诺贝酸主要与葡萄糖醛酸结合，然后随尿液排出。少量非诺贝酸在羰基部分还原为苯甲酰醇代谢物，后者再与葡萄糖醛酸结合并随尿液排出。

In vitro and in vivo metabolism studies reveal that fenofibric acid does not experience significant oxidative metabolism via the cytochrome P450 isoenzymes. The CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 enzymes are not known to play a role in the metabolism of fenofibric acid. Rather, fenofibric acid is predominantly conjugated with glucuronic acid and then excreted in urine. A small amount of fenofibric acid is reduced at the carbonyl moiety to benzhydrol metabolite which is, in turn, conjugated with glucuronic acid and excreted in urine.

来源:DrugBank

代谢

非诺贝酸已知的人类代谢物包括非诺贝醇葡萄糖苷酸。

Fenofibric Acid has known human metabolites that include Fenofibryl glucuronide.

来源:NORMAN Suspect List Exchange

毒理性

• 药物性肝损伤

药品：非诺贝特酸

Compound:fenofibric acid

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注解：模糊的 DILI 关注

DILI Annotation:Ambiguous DILI-concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

严重程度等级：2

Severity Grade:2

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

标签部分：警告和预防措施

Label Section:Warnings and precautions

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

吸收、分配和排泄

• 吸收

一些研究表明，非诺贝酸（给健康志愿者口服130毫克悬浮液，在轻食早餐后约4小时）的生物利用度在大约81%在胃中，88%在近端小肠，84%在远端小肠，和78%在大肠。然而，在健康志愿者口服非诺贝酸后，药物的中位峰值血药浓度大约在给药后2.5小时出现。此外，服用三片35毫克非诺贝酸片后的暴露情况与服用一片105毫克片剂的情况大致相当。

Some studies have demonstrated that the bioavailability of fenofibric acid (a sample administration of 130 mg oral suspension to healthy volunteers about 4 hours after a light breakfast) is approximately 81% in the stomach, 88% in the proximal small bowel, 84% in the distal small bowel, and 78% in the colon. Nevertheless, following the oral administration of fenofibric acid in healthy volunteers, median peak plasma levels for the drug occurred about 2.5 hours after administration. Moreover, exposure after administration of three 35 mg fenofibric acid tablets is largely comparable to that of one 105 mg tablet.

来源:DrugBank

吸收、分配和排泄

• 消除途径

非诺贝酸代谢物主要在尿液中排出。

Fenofibric acid metabolites are largely excreted in the urine.

来源:DrugBank

吸收、分配和排泄

• 分布容积

非诺贝特酸的分布体积被证明是70.9 +/- 27.5升。

The volume of distribution for fenofibric acid is demonstrated to be 70.9 +/- 27.5 L.

来源:DrugBank

吸收、分配和排泄

• 清除

在五位年龄在77至87岁之间的老年志愿者中，服用单剂量非诺贝特后，非诺贝酸口服清除率为1.2升/小时，这相比于年轻成年人的1.1升/小时有所提高。

In five elderly volunteers aged 77 to 87, the oral clearance of fenofibric acid after a single oral dose of fenofibrate was 1.2 L/h, which compares to 1.1 L/h in young adults.

来源:DrugBank

安全信息

• 危险等级：
  9
• 危险品标志：
  Xn,N
• 安全说明：
  S26,S36/37/39
• 危险类别码：
  R36/37/38
• WGK Germany：
  3
• 海关编码：
  2918990090
• 危险品运输编号：
  UN 3077 9 / PGIII
• 危险标志：
  GHS07,GHS09
• 危险性描述：
  H302,H410
• 危险性防范说明：
  P273,P501
• 储存条件：
  -20°C freezer

SDS

---

SECTION 1: Identification of the substance/mixture and of the company/undertaking
Product identifiers
Product name : Fenofibric acid
REACH No. : A registration number is not available for this substance as the substance
or its uses are exempted from registration, the annual tonnage does not
require a registration or the registration is envisaged for a later
registration deadline.
CAS-No. : 42017-89-0
Relevant identified uses of the substance or mixture and uses advised against
Identified uses : Laboratory chemicals, Manufacture of substances

---

SECTION 2: Hazards identification
Classification of the substance or mixture
Classification according to Regulation (EC) No 1272/2008
Acute toxicity, Oral (Category 4), H302
Acute aquatic toxicity (Category 1), H400
Chronic aquatic toxicity (Category 1), H410
For the full text of the H-Statements mentioned in this Section, see Section 16.
Classification according to EU Directives 67/548/EEC or 1999/45/EC
Xn, N Harmful, Dangerous for the R22, R50/53
environment
For the full text of the R-phrases mentioned in this Section, see Section 16.
Label elements
Labelling according Regulation (EC) No 1272/2008
Pictogram
Signal word Warning
Hazard statement(s)
H302 Harmful if swallowed.
H410 Very toxic to aquatic life with long lasting effects.
Precautionary statement(s)
P273 Avoid release to the environment.
P501 Dispose of contents/ container to an approved waste disposal plant.
Supplemental Hazard none
Statements
Other hazards - none

---

SECTION 3: Composition/information on ingredients
Substances
Formula : C17H15ClO4
Molecular Weight : 318,75 g/mol
CAS-No. : 42017-89-0
EC-No. : 255-626-9
Hazardous ingredients according to Regulation (EC) No 1272/2008
Component Classification Concentration
2-[4-(4-Chlorobenzoyl)phenoxy]-2-methylpropionic acid
CAS-No. 42017-89-0 Acute Tox. 4; Aquatic Acute 1; <= 100 %
EC-No. 255-626-9 Aquatic Chronic 1; H302,
H410
Hazardous ingredients according to Directive 1999/45/EC
Component Classification Concentration
2-[4-(4-Chlorobenzoyl)phenoxy]-2-methylpropionic acid
CAS-No. 42017-89-0 Xn, N, R22 - R50/53 <= 100 %
EC-No. 255-626-9
For the full text of the H-Statements and R-Phrases mentioned in this Section, see Section 16

---

SECTION 4: First aid measures
Description of first aid measures
General advice
Consult a physician. Show this safety data sheet to the doctor in attendance.
If inhaled
If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician.
In case of skin contact
Wash off with soap and plenty of water. Consult a physician.
In case of eye contact
Flush eyes with water as a precaution.
If swallowed
Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.
Most important symptoms and effects, both acute and delayed
The most important known symptoms and effects are described in the labelling (see section 2.2) and/or in
section 11
Indication of any immediate medical attention and special treatment needed
no data available

---

SECTION 5: Firefighting measures
Extinguishing media
Suitable extinguishing media
Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Special hazards arising from the substance or mixture
Carbon oxides, Hydrogen chloride gas
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

---

SECTION 6: Accidental release measures
Personal precautions, protective equipment and emergency procedures
Use personal protective equipment. Avoid dust formation. Avoid breathing vapours, mist or gas. Ensure
adequate ventilation. Avoid breathing dust.
For personal protection see section 8.
Environmental precautions
Prevent further leakage or spillage if safe to do so. Do not let product enter drains. Discharge into the
environment must be avoided.
Methods and materials for containment and cleaning up
Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed
containers for disposal.
Reference to other sections
For disposal see section 13.

---

SECTION 7: Handling and storage
Precautions for safe handling
Avoid contact with skin and eyes. Avoid formation of dust and aerosols.
Provide appropriate exhaust ventilation at places where dust is formed.
For precautions see section 2.2.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Specific end use(s)
Apart from the uses mentioned in section 1.2 no other specific uses are stipulated

---

SECTION 8: Exposure controls/personal protection
Control parameters
Components with workplace control parameters
Exposure controls
Appropriate engineering controls
Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and
at the end of workday.
Personal protective equipment
Eye/face protection
Safety glasses with side-shields conforming to EN166 Use equipment for eye protection tested
and approved under appropriate government standards such as NIOSH (US) or EN 166(EU).
Skin protection
Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique
(without touching glove's outer surface) to avoid skin contact with this product. Dispose of
contaminated gloves after use in accordance with applicable laws and good laboratory practices.
Wash and dry hands.
The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and
the standard EN 374 derived from it.
Body Protection
Complete suit protecting against chemicals, The type of protective equipment must be selected
according to the concentration and amount of the dangerous substance at the specific workplace.
Respiratory protection
For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher
level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges.
Use respirators and components tested and approved under appropriate government standards
such as NIOSH (US) or CEN (EU).
Control of environmental exposure
Prevent further leakage or spillage if safe to do so. Do not let product enter drains. Discharge into
the environment must be avoided.

---

SECTION 9: Physical and chemical properties
Information on basic physical and chemical properties
a) Appearance Form: powder
Colour: white
b) Odour no data available
c) Odour Threshold no data available
d) pH no data available
e) Melting point/freezing no data available
point
f) Initial boiling point and no data available
boiling range
g) Flash point no data available
h) Evapouration rate no data available
i) Flammability (solid, gas) no data available
j) Upper/lower no data available
flammability or
explosive limits
k) Vapour pressure no data available
l) Vapour density no data available
m) Relative density no data available
n) Water solubility no data available
o) Partition coefficient: n- log Pow: 3,895
octanol/water
p) Auto-ignition no data available
temperature
q) Decomposition no data available
temperature
r) Viscosity no data available
s) Explosive properties no data available
t) Oxidizing properties no data available
Other safety information
no data available

---

SECTION 10: Stability and reactivity
Reactivity
no data available
Chemical stability
Stable under recommended storage conditions.
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
Strong oxidizing agents
Hazardous decomposition products
Other decomposition products - no data available
In the event of fire: see section 5

---

SECTION 11: Toxicological information
Information on toxicological effects
Acute toxicity
LD50 Oral - rat - 1.242 mg/kg
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitisation
Germ cell mutagenicity
no data available
Carcinogenicity
IARC: No component of this product present at levels greater than or equal to 0.1% is identified as
probable, possible or confirmed human carcinogen by IARC.
Reproductive toxicity
no data available
Specific target organ toxicity - single exposure
no data available
Specific target organ toxicity - repeated exposure
no data available
Aspiration hazard
no data available
Additional Information
RTECS: UA2453000
To the best of our knowledge, the chemical, physical, and toxicological properties have not been
thoroughly investigated.

---

SECTION 12: Ecological information
Toxicity
no data available
Persistence and degradability
no data available
Bioaccumulative potential
no data available
Mobility in soil
no data available
Results of PBT and vPvB assessment
PBT/vPvB assessment not available as chemical safety assessment not required/not conducted
Other adverse effects
Very toxic to aquatic life with long lasting effects.

---

SECTION 13: Disposal considerations
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company. Dissolve or mix the material
with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber.
Contaminated packaging
Dispose of as unused product.

---

SECTION 14: Transport information
UN number
ADR/RID: 3077 IMDG: 3077 IATA: 3077
UN proper shipping name
ADR/RID: ENVIRONMENTALLY HAZARDOUS SUBSTANCE, SOLID, N.O.S. (2-[4-(4-
Chlorobenzoyl)phenoxy]-2-methylpropionic acid)
IMDG: ENVIRONMENTALLY HAZARDOUS SUBSTANCE, SOLID, N.O.S. (2-[4-(4-
Chlorobenzoyl)phenoxy]-2-methylpropionic acid)
IATA: Environmentally hazardous substance, solid, n.o.s. (2-[4-(4-Chlorobenzoyl)phenoxy]-2-
methylpropionic acid)
Transport hazard class(es)
ADR/RID: 9 IMDG: 9 IATA: 9
Packaging group
ADR/RID: III IMDG: III IATA: III
Environmental hazards
ADR/RID: yes IMDG Marine pollutant: yes IATA: yes
Special precautions for user
Further information
EHS-Mark required (ADR 2.2.9.1.10, IMDG code 2.10.3) for single packagings and combination
packagings containing inner packagings with Dangerous Goods > 5L for liquids or > 5kg for solids.

---

---

SECTION 15 - REGULATORY INFORMATION
N/A

---

SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

副作用 非诺贝特胶囊是常见的剂型之一。非诺贝特可能引起肝脏和肾脏损伤，并伴有胃肠道不适等症状。

长期服用非诺贝特会使转氨酶升高，损害肝功能；严重情况下，还可能导致肾功能衰竭、胆囊结石及肌肉损伤等副作用。因此，长期服药者应定期检查肝肾功能，如有异常应及时减量或停药。

此外，非诺贝特还会引起胃肠道不适，如腹痛、腹泻和便秘等症状。患者在使用时应注意复查肝功能和肌酶谱，并保持低脂饮食及规律运动。该药物对药物过敏者禁用，严重肝肾功能不全者亦禁用，儿童慎用。

生物活性 非诺贝特酸（Fenofibric acid）是一种降脂剂，能够降低低密度脂蛋白胆固醇和甘油三酯水平。其作为PPARα激动剂，具有提高高密度脂蛋白的效果，并能增强脂肪酸分解代谢、降低血脂水平——主要是甘油三酯。

靶点 表1. 靶点

• PPARα

体外研究 纤维酸类药物是降脂药的活化形式，也是PPARα的激动剂。它们通过提高ABCA1表达和apoA-I介导的HDL生成来增强脂肪酸分解代谢，并降低血脂水平——尤其是甘油三酯。纤维酸还通过增强依赖于LXR的ABCA1基因转录来发挥其对ABCA1表达的作用。

体内研究 非诺贝特酸减弱了OIR小鼠循环内皮祖细胞（EPC）的异常增多，这依赖于PPARα。它抑制低氧诱导的视网膜内皮祖细胞增多、减少循环中CXCR4阳性EPC的数量，并下调血清SDF-1水平及抑制视网膜中HIF-1a和SDF-1的过表达。

用途

• 用作医药中间体。
• 非诺贝特的中间体。
• Fenofibric acid是Fenofibrate（F248640）的活性代谢物，通过肝X受体依赖的方式增强ABCA1基因转录，增加Apoliprotein A-I介导的HDL生物生成。

反应信息

• 作为反应物：
  描述：

  非诺贝特酸 在 硼烷四氢呋喃络合物 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 以94%的产率得到2-(4-((4-chlorophenyl)(hydroxy)methyl)phenoxy)-2-methylpropan-1-ol
  参考文献：
  名称：

  DRUG DERIVATIVES

  摘要：

  本发明涉及已知活性药物化合物的衍生物。这些衍生物通过是活性化合物的氧化还原衍生物与母体活性化合物相区别。这意味着活性化合物中的一个或多个官能团已转化为另一组，在一项或多项反应中，这可以被认为代表氧化态的变化。我们通常将这些化合物称为氧化还原衍生物。发明中的衍生物可能与原始母体活性药物化合物仅通过单一步骤转换有关，或者可能通过包括一个或多个氧化态变化的几个合成步骤与之相关。在某些情况下，经过两个或更多转换后获得的官能团可能与母体活性化合物处于相同的氧化态（我们将这些化合物包括在我们的氧化还原衍生物定义中）。在其他情况下，发明的衍生物的氧化态可以被认为是与母体化合物不同的。在许多情况下，发明中的化合物本身就具有固有的治疗活性。在某些情况下，相对于母体化合物的相同靶点或靶点，这种活性与母体化合物针对该靶点或靶点的活性一样好或更好。

  公开号：

  US20130225594A1
• 作为产物：
  描述：

  非诺贝特杂质E 在 lithium hydroxide 作用下， 以 甲醇 、 水 为溶剂， 以0.95 g的产率得到非诺贝特酸
  参考文献：
  名称：

  非诺贝特半抗原及其制备方法、非诺贝特抗原、抗体及其用途

  摘要：

  本发明公开了一种非诺贝特半抗原，其具有式(I)所述的结构式。本发明还涉及非诺贝特抗原、非诺贝特抗体及其包含该非诺贝特抗原和该非诺贝特抗体的试纸条的快速检测装置及其和应用。本发明的试纸条能够实现非诺贝特的即时检测，检测时间仅需数分钟，且不需要大型仪器设备以及复杂的实验步骤，结果易判断，适用性强，成本低、易推广使用，非常适合于基层食品安全监管部门进行非诺贝特的快速检测。

  公开号：

  CN115124424A

文献信息

• [EN] SULFONYL COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN<br/>[FR] COMPOSÉS DE SULFONYLE QUI INTERAGISSENT AVEC LA PROTÉINE RÉGULATRICE DE LA GLUCOKINASE
  申请人：AMGEN INC

  公开号：WO2013123444A1

  公开（公告）日：2013-08-22

  The present invention relates to sulfonyl compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

  本发明涉及与葡萄糖激酶调节蛋白相互作用的磺酰基化合物。此外，本发明涉及使用这些化合物或其药学上可接受的盐治疗2型糖尿病和其他涉及葡萄糖激酶调节蛋白的疾病和/或症状的方法，以及含有这些化合物或其药学上可接受的盐的药物组合物。
• [EN] METHYL OXAZOLE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] MÉTHYLOXAZOLES ANTAGONISTES DU RÉCEPTEUR DE L'OREXINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2016089721A1

  公开（公告）日：2016-06-09

  The present invention is directed to methyl oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及甲基噁唑化合物，其为促进睡眠的受体拮抗剂。本发明还涉及所述化合物在潜在治疗或预防涉及促进睡眠的神经和精神疾病和疾病中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在预防或治疗涉及促进睡眠的疾病中的用途。
• 3-Aminocyclopentanecarboxamides as modulators of chemokine receptors
  申请人：Xue Chu-Biao

  公开号：US20060004018A1

  公开（公告）日：2006-01-05

  The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.

  本发明涉及以下式的化合物： 这些化合物是趋化因子受体的调节剂。本发明的化合物及其组合物在治疗与趋化因子受体表达和/或活性相关的疾病方面是有用的。
• Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors
  申请人：Goble D. Stephen

  公开号：US20070238723A1

  公开（公告）日：2007-10-11

  Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.

  环戊基化合物通过酰胺基团与苯并噁唑基团相连，利用苯并噁唑环的环氮原子，并进一步用杂环基团取代，这些化合物由式I表示： 用于调节CCR-2趋化因子受体，以预防或治疗炎症和免疫调节性疾病和疾病，过敏性疾病，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及类风湿性关节炎和动脉粥样硬化等自身免疫病理病变；以及包含这些化合物的药物组合物和这些化合物和组合物的使用。
• Cleavage of Carboxylic Esters by Aluminum and Iodine
  作者：Dayong Sang、Huaxin Yue、Yang Fu、Juan Tian

  DOI：10.1021/acs.joc.1c00034

  日期：2021.3.5

  A one-pot procedure for deprotecting carboxylic esters under nonhydrolytic conditions is described. Typical alkyl carboxylates are readily deblocked to the carboxylic acids by the action of aluminum powder and iodine in anhydrous acetonitrile. Cleavage of lactones affords the corresponding ω-iodoalkylcarboxylic acids. Aryl acetylates undergo deacetylation with the participation of the neighboring group

  描述了一种在非水解条件下使羧酸酯脱保护的一锅法方法。在无水乙腈中，铝粉和碘的作用下，典型的羧酸烷基酯很容易解封为羧酸。切割内酯得到相应的ω-碘代烷基羧酸。乙酸芳基酯在相邻基团的参与下进行脱乙酰化。该方法能够在芳基酯存在下选择性裂解烷基羧酸酯。