对氯苯乙酰氯 | 25026-34-0

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物 - 羧酸酰卤化物
• 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: 对氯苯乙酰氯
• 中文别名: 4-氯苯乙酰氯；4-氯苯基乙酰氯；4-氯苯基乙酰基氯
• 英文名称: 4-chlorophenacetyl chloride
• 英文别名: 4-chlorophenylacetyl chloride；2-(4-chlorophenyl)acetyl chloride；p-chlorophenyl acetyl chloride
• CAS: 25026-34-0
• 化学式: C₈H₆Cl₂O
• mdl: MFCD00037111
• 分子量: 189.041
• InChiKey: UMQUIRYNOVNYPA-UHFFFAOYSA-N

物化性质

• 比旋光度：
  -56.7 º
• 沸点：
  85 °C1 mm Hg(lit.)
• 密度：
  1.292 g/mL at 25 °C(lit.)
• 闪点：
  >230 °F
• 稳定性/保质期：
  如果按照规格使用和储存，则不会分解。请避免接触氧化物、水分或潮湿环境。

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  17.1
• 氢给体数：
  0
• 氢受体数：
  1

安全信息

• 危险等级：
  8
• 危险品标志：
  C
• 安全说明：
  S24/25,S26,S36/37/39,S45
• 危险类别码：
  R34
• WGK Germany：
  3
• 海关编码：
  2916399090
• 包装等级：
  II
• 危险类别：
  8
• 危险品运输编号：
  UN 3265 8/PG 2
• 危险性防范说明：
  P260,P261,P264,P270,P271,P280,P301+P312,P301+P330+P331,P302+P352,P303+P361+P353,P304+P340,P305+P351+P338,P310,P312,P321,P322,P330,P363,P405,P501
• 危险性描述：
  H302,H312,H314,H332
• 储存条件：
  在干性保护气体中处理，并确保贮藏容器密封。将其存放在紧密封装的容器中，并存放于阴凉、干燥处。

SDS

Name:	4-Chlorobenzeneacetyl chloride 98% Material Safety Data Sheet
Synonym:	4-Chlorophenylacetyl chloride
CAS:	25026-34-0

Section 1 - Chemical Product MSDS Name:4-Chlorobenzeneacetyl chloride 98% Material Safety Data Sheet
Synonym:4-Chlorophenylacetyl chloride

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Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS

CAS#	Chemical Name	content	EINECS#
25026-34-0	4-Chlorobenzeneacetyl chloride, 98%	98	246-571-1

Hazard Symbols: C
Risk Phrases: 34

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Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
Causes burns.Corrosive.
Potential Health Effects
Eye:
Causes eye burns. May cause chemical conjunctivitis and corneal damage.
Skin:
Causes skin burns. May cause skin rash (in milder cases), and cold and clammy skin with cyanosis or pale color.
Ingestion:
May cause severe and permanent damage to the digestive tract. Causes gastrointestinal tract burns. May cause perforation of the digestive tract. May cause systemic effects.
Inhalation:
May cause severe irritation of the respiratory tract with sore throat, coughing, shortness of breath and delayed lung edema. Causes chemical burns to the respiratory tract. Aspiration may lead to pulmonary edema. May cause systemic effects.
Chronic:
Effects may be delayed.

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Section 4 - FIRST AID MEASURES
Eyes: Get medical aid immediately. Do NOT allow victim to rub eyes or keep eyes closed. Extensive irrigation with water is required (at least 30 minutes).
Skin:
Get medical aid immediately. Immediately flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Wash clothing before reuse. Destroy contaminated shoes.
Ingestion:
Do not induce vomiting. If victim is conscious and alert, give 2-4 cupfuls of milk or water. Never give anything by mouth to an unconscious person. Get medical aid immediately.
Inhalation:
Get medical aid immediately. Remove from exposure and move to fresh air immediately. If breathing is difficult, give oxygen. Do NOT use mouth-to-mouth resuscitation. If breathing has ceased apply artificial respiration using oxygen and a suitable mechanical device such as a bag and a mask.
Notes to Physician:

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Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion. Vapors may be heavier than air. They can spread along the ground and collect in low or confined areas.
Extinguishing Media:
In case of fire, use water, dry chemical, chemical foam, or alcohol-resistant foam. Use agent most appropriate to extinguish fire.

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Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Absorb spill with inert material (e.g. vermiculite, sand or earth), then place in suitable container. Clean up spills immediately, observing precautions in the Protective Equipment section. Provide ventilation.

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Section 7 - HANDLING and STORAGE
Handling:
Remove contaminated clothing and wash before reuse. Use only in a well-ventilated area. Do not breathe dust, vapor, mist, or gas. Do not get in eyes, on skin, or on clothing. Keep container tightly closed. Do not ingest or inhale. Discard contaminated shoes.
Storage:
Keep container closed when not in use. Store in a tightly closed container. Store in a cool, dry, well-ventilated area away from incompatible substances. Corrosives area.

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Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use adequate ventilation to keep airborne concentrations low.
Exposure Limits CAS# 25026-34-0: Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear appropriate protective clothing to prevent skin exposure.
Respirators:
A respiratory protection program that meets OSHA's 29 CFR 1910.134 and ANSI Z88.2 requirements or European Standard EN 149 must be followed whenever workplace conditions warrant respirator use.

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Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Liquid
Color: red-pink
Odor: None reported.
pH: Not available.
Vapor Pressure: Not available.
Viscosity: Not available.
Boiling Point: Not available.
Freezing/Melting Point: Not available.
Autoignition Temperature: Not applicable.
Flash Point: Not applicable.
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature:
Solubility in water:
Specific Gravity/Density:
Molecular Formula: C8H6Cl2O
Molecular Weight: 189.04

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Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Stable under normal temperatures and pressures.
Conditions to Avoid:
Incompatible materials, excess heat.
Incompatibilities with Other Materials:
Strong oxidizing agents.
Hazardous Decomposition Products:
Hydrogen chloride, carbon monoxide, irritating and toxic fumes and gases, carbon dioxide.
Hazardous Polymerization: Has not been reported.

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Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 25026-34-0 unlisted.
LD50/LC50:
Not available.
Carcinogenicity:
4-Chlorobenzeneacetyl chloride, 98% - Not listed by ACGIH, IARC, or NTP.

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Section 12 - ECOLOGICAL INFORMATION

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Section 13 - DISPOSAL CONSIDERATIONS
Dispose of in a manner consistent with federal, state, and local regulations.

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Section 14 - TRANSPORT INFORMATION

IATA
Shipping Name: CORROSIVE LIQUID, ACIDIC, ORGANIC, N.O.S.
Hazard Class: 8
UN Number: 3265
Packing Group: II
IMO
Shipping Name: CORROSIVE LIQUID, ACIDIC, ORGANIC, N.O.S.
Hazard Class: 8
UN Number: 3265
Packing Group: II
RID/ADR
Shipping Name: CORROSIVE LIQUID, ACIDIC, ORGANIC, N.O.S.
Hazard Class: 8
UN Number: 3265
Packing group: II

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Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: C
Risk Phrases:
R 34 Causes burns.
Safety Phrases:
S 24/25 Avoid contact with skin and eyes.
WGK (Water Danger/Protection)
CAS# 25026-34-0: No information available.
Canada
None of the chemicals in this product are listed on the DSL/NDSL list.
CAS# 25026-34-0 is not listed on Canada's Ingredient Disclosure List.
US FEDERAL
TSCA
CAS# 25026-34-0 is not listed on the TSCA inventory.
It is for research and development use only.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

化学性质：沸点为120℃，折光率为1.55至1.552。

反应信息

• 作为反应物：
  描述：

  对氯苯乙酰氯 在 cesium acetate 作用下， 以 乙醚 、 乙醇 、 水 为溶剂， 反应 8.13h， 生成 2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid
  参考文献：
  名称：

  Methods and Compositions for Treatment of Scleritis and Related Disorders

  摘要：

  目前的教导涉及抗炎物质领域，更具体地涉及对用于治疗巩膜炎、巩膜炎症状或与巩膜炎相关疾病有用的化合物。在一个方面，治疗巩膜炎、巩膜炎症状或巩膜炎相关疾病的方法通常包括向受试者施用公式I的化合物： 或其药用可接受的盐、水合物或酯，其中W 1 ，W 2 ，R 1 ，L，X，Y，Z和n 1 的定义如本文所述。

  公开号：

  US20080125454A1
• 作为产物：
  描述：

  对氯苯乙酸 在 草酰氯 作用下， 以 氯仿 为溶剂， 生成 对氯苯乙酰氯
  参考文献：
  名称：

  （2S）-1-（芳基乙酰基）-2-（氨基甲基）哌啶衍生物：新颖的高选择性κ阿片类镇痛药。

  摘要：

  本文描述了新型的1-（芳基乙酰基）-2-（氨基甲基）哌啶衍生物的合成和构效关系，作为κ阿片类镇痛药。通过计算研究和1H NMR定义了具有60度扭转角（N1C2C7N8）的药效团的活性构象。芳香族部分取代的定量结构-活性关系研究表明，对位和/或间位存在吸电子和亲脂性取代基是良好的镇痛活性和κ亲和力所必需的。铅化合物（2S）-1-[（（3,4-二氯苯基）乙酰基] -2-（吡咯烷-1-基甲基）哌啶盐酸盐和（2S）-1- [4-（三氟甲基）苯基]乙酰基] -2 -（吡咯烷-1-基甲基）哌啶盐酸盐的Kappa / mu选择性最高（分别为6500：1和4100：1）以及迄今为止鉴定出的最有力的（κκ0.24和0.57 nM）κ配体。在抗伤害感受的小鼠甩尾模型中，化合物14（ED50 = 0.05 mg / kg sc）的效力是吗啡的25倍，效力是标准Kappa配体U-50488的16倍。

  DOI：

  10.1021/jm00105a061
• 作为试剂：
  描述：

  庚胺 、 苄基二异丙基胺 、 对氯苯乙酰氯 在 氮气 、 对氯苯乙酰氯 、 NH2 、 乙腈 、 acetonitrile-water 、 乙酸铵 、 乙酸乙酯 、 Brine 、 magnesium sulfate 作用下， 反应 16.5h， 以to give 1.045 g of 2-(4-chlorophenyl)-N-heptylacetamide (yield 45.0%)的产率得到2-(4-chlorophenyl)-N-heptylacetamide
  参考文献：
  名称：

  Benzoic acid derivatives as modulators of ppar alpha and gamma

  摘要：

  化合物的式子为(I)，其中R1表示芳基，可选地被杂环基取代，或者是可选地被芳基取代的杂环基，其中每个芳基或杂环基都可以被取代; 在苯环中，基团—CH2)m-T-(CH2)n—U—(CH2)p—以式(I)中的数字所示的3或4位置附着，并表示从以下一种或多种中选择的基团：O(CH2)2、O(CH2)3、NC(O)NR4(CH2)2、CH2S(O2)NR5(CH2)2、CH2N(R6)C(O)CH2、(CH2)2N(R6)C(O)(CH2)2、C(O)NR7CH2、C(O)NR7(CH2)2和CH2N(R6)C(O)CH2O; V表示O、S、NR8或单键; q表示1、2或3; W表示O、S、N(R9)C(O)、NR10或单键; R2表示卤素、可选地被一个或多个氟代取代的C1-4烷基、可选地被一个或多个氟代取代的C1-4烷氧基、C1-4酰基、芳基、芳基C1-4烷基、CN或NO2; r表示0、1、2或3; R3表示卤素、可选地被一个或多个氟代取代的C1-4烷基、可选地被一个或多个氟代取代的C1-4烷氧基、C1-4酰基、芳基、芳基C1-4烷基或CN; s表示0、1、2或3; R4、R5、R6、R7、R8、R9和R10独立地表示H、C1-10烷基、芳基或芳基C1-4烷基，或者当m为0且T表示一个基团N(R6)C(O)或一个基团(R5)NS(O2)时，R1和R或R1和R5与它们附着的氮原子一起表示杂芳基; 具有附加条件和药学上可接受的盐，制备这种化合物的过程，它们在治疗与胰岛素抵抗相关的临床病症方面的用途，它们的治疗用途的方法以及包含它们的制药组合物。

  公开号：

  US20050267149A1

文献信息

• Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists
  申请人：Failli A. Amedeo

  公开号：US20060287522A1

  公开（公告）日：2006-12-21

  This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).

  这项发明提供了从式（1）中选择的吡咯苯并二氮杂吡咯烷吡啶羧酰胺，其作为卵泡刺激素受体拮抗剂。该发明还提供了利用式（1）和（2）化合物的药物组合物和治疗方法。
• Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABAA1 receptor with potent anticonvulsant activity and low toxicity
  作者：Longjiang Huang、Jing Ding、Min Li、Zhipeng Hou、Yanru Geng、Xiufen Li、Haibo Yu

  DOI：10.1016/j.ejmech.2019.111824

  日期：2020.1

  antiepileptic drugs, a series of 2,5-disubstituted [1,2,4]-triazolo[1,5-a]pyrimidine-7(4H)-one derivatives were designed and synthesized. Spontaneous Ca2+ oscillations (SCOs) of cortical neurons were used for in vitro phenotypic screening. Maximal electroshock test (MES) and pentylenetetrazole (PTZ) test were used to access their anticonvulsant activity, and rotarod test was used to estimate their neurotoxicity

  为了寻找更有效，更安全的抗癫痫药，设计并合成了一系列2,5-二取代的[1,2,4]-三唑并[1,5-a]嘧啶-7（4H）-one衍生物。皮层神经元的自发Ca 2+振荡（SCO）用于体外表型筛选。使用最大电击试验（MES）和戊四唑（PTZ）试验来获得其抗惊厥活性，并使用rotarod试验评估其神经毒性。体外模型中的活性化合物在戊四氮（PTZ）诱发的癫痫模型中特别有效，但在最大电击（MES）模型中无效，与常用药物相比，更重要的是具有较低的神经毒性。其中，化合物5c和5e在PTZ诱发的癫痫模型中显示出显着的抗惊厥活性，ED50值分别为31.81 mg / kg和40.95 mg / kg，分别。这些化合物具有改善的神经毒性，其保护指数（PI = TD50 / ED50）值分别为17.22和9.09。最后，我们证明了化合物5c和5e主要作为正调节剂作用于GABAA受体，但没有钠通道。因此，本研究为癫痫的进一步研究提供了潜在的候选者。
• Substituted alkyl amido piperidines
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US20040186103A1

  公开（公告）日：2004-09-23

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.

  这项发明涉及选择性拮抗黑色素浓缩激素-1（MCH1）受体的化合物。该发明提供了一种包括该发明化合物的治疗有效量和药学上可接受的载体的药物组合物。该发明提供了一种由结合本发明化合物的治疗有效量和药学上可接受的载体制成的药物组合物。该发明还提供了一种制备药物组合物的方法，包括结合本发明化合物的治疗有效量和药学上可接受的载体。该发明还提供了一种减少受试者体重的方法，包括向受试者施用本发明化合物的有效量以减少受试者的体重。该发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，包括向受试者施用本发明化合物的有效量以治疗受试者的抑郁症和/或焦虑症。
• [EN] SUBSTITUTED BENZAMIDE DERIVATIVES<br/>[FR] DÉRIVÉS DE BENZAMIDE SUBSTITUÉS
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011076678A1

  公开（公告）日：2011-06-30

  The invention relates to compounds of formula I wherein R is hydrogen or lower alkyl; R1 is -(CH2)n-(O)o-heterocycloalkyl or -C(O)-heterocycloalkyl, wherein the heterocycloalkyl group is optionally substituted by lower alkyl, hydroxy, halogen or by -(CH2)p-aryl; n is 0, 1 or 2; o is 0 or 1; p is 0, 1 or 2; R2 is CF3, cycloalkyl, optionally substituted by lower alkoxy or halogen, or is indan-2-yl, or is heterocycloalkyl, optionally substituted by heteroaryl, or is aryl or heteroaryl, wherein the aromatic rings are optionally substituted by one or two substituents, selected from lower alkyl, halogen, heteroaryl, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2C1)(CH3), S-lower alkyl, lower alkoxy, CH2-lower alkoxy, lower alkinyl or cyano, or by-C(O)-phenyl, -O-phenyl, -O- CH2-phenyl, phenyl or -CH2-phenyl, and wherein the phenyl rings may optionally be substituted by halogen, -C(O)-lower alkyl, -C(O)OH or -C(O)O-lower alkyl, or the aromatic rings are optionally substituted by heterocycloalkyl, OCH2-oxetan-3-yl or O-tetrahydropyran-4-yl, optionally substituted by lower alkyl; X is a bond, -NR'-, -CH2NH-, -CHR''-, -(CHR'')q-O-, -O-(CHR'')q- or -(CH2)2-; Y is a bond or -CH2- R' is hydrogen or lower alkyl, R'' is hydrogen, lower alkyl, CF3, lower alkoxy, q is 0, 1, 2 or 3; or to a pharmaceutically suitable acid addition salt thereof. It has now been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinsons disease, neurodegenerative disorders such as Alzheimers disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

  该发明涉及以下式I的化合物，其中R是氢或较低的烷基；R1是-(CH2)n-(O)o-杂环烷基或-C(O)-杂环烷基，其中杂环烷基基团可选择地被较低的烷基，羟基，卤素或-(CH2)p-芳基取代；n为0、1或2；o为0或1；p为0、1或2；R2为CF3，环烷基，可选择地被较低的烷氧基或卤素取代，或为茚-2-基，或为杂环烷基，可选择地被杂芳基取代，或为芳基或杂芳基，其中芳香环可选择地被来自较低的烷基，卤素，杂芳基，羟基，CF3，OCF3，OCH2CF3，OCH2-环烷基，OCH2C(CH2OH)(CH2C1)(CH3)，S-较低的烷基，较低的烷氧基，CH2-较低的烷氧基，较低的炔基或氰基，或-C(O)-苯基，-O-苯基，-O-CH2-苯基，苯基或-CH2-苯基选择的一个或两个取代基取代，其中苯环可选择地被卤素，-C(O)-较低的烷基，-C(O)OH或-C(O)O-较低的烷基取代，或芳香环可选择地被杂环烷基，OCH2-氧杂环戊烷-3-基或O-四氢吡喃-4-基，可选择地被较低的烷基取代；X为键，-NR'-，-CH2NH-，-CHR''-，-(CHR'')q-O-，-O-(CHR'')q-或-(CH2)2-；Y为键或-CH2-；R'为氢或较低的烷基，R''为氢，较低的烷基，CF3，较低的烷氧基，q为0、1、2或3；或其药学上适宜的酸盐。现已发现，该式I的化合物对痕量胺相关受体（TAARs）具有良好的亲和力，特别是对于TAAR1。这些化合物可用于治疗抑郁症，焦虑症，躁郁症，注意力缺陷多动障碍（ADHD），与压力有关的疾病，如精神分裂症，帕金森病等神经疾病，阿尔茨海默病等神经退行性疾病，癫痫，偏头痛，高血压，物质滥用和代谢性疾病，如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和吸收异常，体温稳态异常，睡眠和昼夜节律异常，以及心血管疾病。
• Design, Synthesis, and Biological Evaluation of New 8-Heterocyclic Xanthine Derivatives as Highly Potent and Selective Human A_2B Adenosine Receptor Antagonists
  作者：Pier Giovanni Baraldi、Mojgan Aghazadeh Tabrizi、Delia Preti、Andrea Bovero、Romeo Romagnoli、Francesca Fruttarolo、Naser Abdel Zaid、Allan R. Moorman、Katia Varani、Stefania Gessi、Stefania Merighi、Pier Andrea Borea

  DOI：10.1021/jm0309654

  日期：2004.3.1

  in radioligand binding assays at human (h) A(1), A(2A), A(2B), and A(3) ARs. We introduced several heterocycles, such as pyrazole, isoxazole, pyridine, and pyridazine, at the 8-position of the xanthine nucleus and we have also investigated different spacers (substituted acetamide, oxyacetamide, and urea moieties) on the heterocycle introduced. Various groups at the 3- and 4-positions of phenylacetamide

  在这里，我们报告8杂环取代的黄嘌呤作为有效和选择性A（2B）腺苷受体拮抗剂的合成。探索了黄嘌呤与重组人A（2B）腺苷受体（ARs）结合在HEK-293细胞（HEK-A（2B））和其他AR亚型中的结构活性关系（SAR）。合成的化合物在纳摩尔浓度范围内显示出A（2B）腺苷受体亲和力，并且在人类（h）A（1），A（2A），A（2B）和A（3）的放射性配体结合测定中评估了良好的选择性水平AR。我们在黄嘌呤核的8位引入了几个杂环，例如吡唑，异恶唑，吡啶和哒嗪，我们还研究了所引入杂环上的不同间隔基（取代的乙酰胺，氧乙酰胺和脲部分）。研究了苯基乙酰胺部分的3位和4位上的各种基团。这项研究使我们能够确定衍生物2-（3,4-二甲氧基苯基）-N- [5-（2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin- 8-基）-1-甲基-1H-吡唑-3-基]乙酰胺（29

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