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医药中间体

医药中间体是指在药物合成过程中作为关键步骤的反应产物或原料物质,它们通常是化学结构较为简单的化合物,通过一系列化学反应可以转化为最终的药物成品。这些中间体在制药工业中扮演着重要角色,是实现复杂药物分子合成的关键组成部分。

特点
  1. 多样性:医药中间体种类繁多,根据所需药品的不同而不同。
  2. 复杂性:有些医药中间体本身可能较为简单,但通过一系列复杂的化学反应才能获得最终的药物成品。
  3. 安全性与纯度要求高:在制药行业中,医药中间体的安全性和纯度直接影响到最终产品的质量和效果。
应用
  1. 合成新药:许多复杂结构的新药都是通过一些简单的中间体经过一系列复杂的化学反应而合成得到的。
  2. 药物改良:通过对现有药物中的某些关键中间体进行优化,可以开发出更有效的治疗手段或者降低副作用。
  3. 原料供应保障:确保医药中间体的稳定供应对于维持药品市场供给至关重要。
生产与研发

医药中间体的研发和生产是一个复杂的过程,通常包括以下几个步骤:

  • 合成设计:根据目标药物结构设计合适的合成路线。
  • 实验室规模合成与优化:通过小规模实验来验证并优化反应条件。
  • 中试放大:将实验室中的成功方案应用于工业化生产前的中间试验阶段。
  • 工业化生产:在确保安全性和质量的前提下进行大规模生产。
发展趋势

随着化学合成技术的进步和新技术的应用(如绿色化学、计算机辅助设计等),医药中间体的研发与生产正朝着更加高效、环保的方向发展。同时,对药物分子结构的深入理解也为开发更有效的治疗方案提供了更多可能性。

中文名称 英文名称 CAS号 化学式 结构式图片
—— (+/-)-phenylmethyl 3-(aminomethyl)-3-hydroxy-1-pyrrolidinecarboxylate 872715-55-4 C13H18N2O3
(+/-)-phenylmethyl 3-(aminomethyl)-3-hydroxy-1-pyrrolidinecarboxylate
—— 5-bromo-6-methoxy-1,3-dimethyl-1H-pyrimidine-2,4-dione 851608-69-0 C7H9BrN2O3
5-bromo-6-methoxy-1,3-dimethyl-1H-pyrimidine-2,4-dione
—— 4-oxo-4-thiophen-2-yl-but-2-enoic acid 37992-45-3 C8H6O3S
4-oxo-4-thiophen-2-yl-but-2-enoic acid
—— methyl 3-chloroquinoline-6-carboxylate 1357958-20-3 C11H8ClNO2
methyl 3-chloroquinoline-6-carboxylate
—— 3(2H)-Pyridazinone, 6-(m-methoxyphenyl)-4-methyl-2-(2-morpholinoethyl)-, hydrochloride 13299-99-5 C18H24ClN3O3
3(2H)-Pyridazinone, 6-(m-methoxyphenyl)-4-methyl-2-(2-morpholinoethyl)-, hydrochloride
—— 2-Deoxystreptamine 2037-48-1 C6H14N2O3
2-Deoxystreptamine
—— N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine 295330-45-9 C22H25ClFN5O2
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine
—— 4-(trifluoromethoxy)piperidine 1206984-05-5 C6H10F3NO
4-(trifluoromethoxy)piperidine
—— 2-Benzyl-2,3-dihydro-4(1H)-isochinolon 53667-19-9 C16H15NO
2-Benzyl-2,3-dihydro-4(1H)-isochinolon
—— 4-(4-methyl-2-pyrimidinyl)benzaldehyde 433920-95-7 C12H10N2O
4-(4-methyl-2-pyrimidinyl)benzaldehyde
—— Bromadol HCL BDPC 77239-98-6 C22H28BrNO
Bromadol HCL BDPC
—— 5,7,12,14-tetrahydro-5,7,12,14-tetraazapentacene 162039-67-0 C18H14N4
5,7,12,14-tetrahydro-5,7,12,14-tetraazapentacene
—— 3,6-bis(5-bromopyridin-2-yl)-2,5-bis(2-octyldodecyl)pyrrolo[3,4-c]pyrrole-1,4(2H,5H)-dione 1455028-34-8 C56H88Br2N4O2
3,6-bis(5-bromopyridin-2-yl)-2,5-bis(2-octyldodecyl)pyrrolo[3,4-c]pyrrole-1,4(2H,5H)-dione
—— 3-methyl-[1,2,4]oxadiazole-5-carboxylic acid potassium salt 1240605-84-8 C4H3N2O3*K
3-methyl-[1,2,4]oxadiazole-5-carboxylic acid potassium salt
—— Diphenyl azodicarboxylate 2449-14-1 C14H10N2O4
Diphenyl azodicarboxylate
—— (±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester 172336-32-2 C27H28FNO4
(±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester
—— sodium sulfamethoxypyridazinato 2577-32-4 C11H11N4O3S*Na
sodium sulfamethoxypyridazinato
—— N-Methyl-cis-2,5-dimethyl-piperazin 1152368-00-7 C7H16N2
N-Methyl-cis-2,5-dimethyl-piperazin
—— 3-ethynyl-2-methylbenzo[b]thiophene 1300021-13-9 C11H8S
3-ethynyl-2-methylbenzo[b]thiophene
—— 1-(4-Benzylamino-piperidin-1-yl)-ethanone 577778-36-0 C14H20N2O
1-(4-Benzylamino-piperidin-1-yl)-ethanone
—— 4-chloro-2-(chloromethyl)pyrimidine 3842-28-2 C5H4Cl2N2
4-chloro-2-(chloromethyl)pyrimidine
—— 7-bromo-3,3-dibutyl-8-hydroxy-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepine 1,1-dioxide 358376-04-2 C23H30BrNO3S
7-bromo-3,3-dibutyl-8-hydroxy-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepine 1,1-dioxide
—— 1,4-bis(dimethoxymethylsilyl)benzene 135778-06-2 C12H22O4Si2
1,4-bis(dimethoxymethylsilyl)benzene
—— bis-1,3-(4-aminobenzamido)benzene 2362-25-6 C20H18N4O2
bis-1,3-(4-aminobenzamido)benzene
—— 2,7-dibromo-4,9-dihydro-4,4,9,9-tetrahexadecyl-s-indaceno[1,2-b:5,6-b']-dithiophene 1209012-35-0 C80H136Br2S2
2,7-dibromo-4,9-dihydro-4,4,9,9-tetrahexadecyl-s-indaceno[1,2-b:5,6-b']-dithiophene
—— 7-methylisoquinolin-1-amine 950768-74-8 C10H10N2
7-methylisoquinolin-1-amine
—— 4-hydroxy-5-chloro-6-(1-fluoroethyl)pyrimidine 227184-12-5 C6H6ClFN2O
4-hydroxy-5-chloro-6-(1-fluoroethyl)pyrimidine
—— 6-(1-fluoroethyl)-5-iodo-4-pyrimidone 438449-92-4 C6H6FIN2O
6-(1-fluoroethyl)-5-iodo-4-pyrimidone
—— 5'-Amino-3,4,5,6-tetrahydro-[1,2']bipyridinyl-2-one 444002-72-6 C10H13N3O
5'-Amino-3,4,5,6-tetrahydro-[1,2']bipyridinyl-2-one
—— 2-[2-(4-chlorophenyl)ethenyl]quinoline 38101-91-6 C17H12ClN
2-[2-(4-chlorophenyl)ethenyl]quinoline
—— 5-chloropyridin-3-yl 1H-indole-4-carboxylate 1087243-14-8 C14H9ClN2O2
5-chloropyridin-3-yl 1H-indole-4-carboxylate
—— (+/-)-coronaridine 467-77-6 C21H26N2O2
(+/-)-coronaridine
—— 2,5-dimethylpyrrolidine hydrochloride 63639-02-1 C6H13N*ClH
2,5-dimethylpyrrolidine hydrochloride
—— 6-chloronicotinoyl chloride 58757-38-3 C10H10Cl2N2O
6-chloronicotinoyl chloride
—— (R)-3-(4-bromophenyl)piperidine 1336754-69-8 C11H14BrN
(R)-3-(4-bromophenyl)piperidine
—— 3-(3,5-dichloro-4-hydroxybenzoyl)-1-oxo-2,3-dihydro-1,3-benzothiazole 1285572-55-5 C14H9Cl2NO3S
3-(3,5-dichloro-4-hydroxybenzoyl)-1-oxo-2,3-dihydro-1,3-benzothiazole
—— 5-chloro-2-cyclopropyl-1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid 858956-26-0 C8H7ClN2O3
5-chloro-2-cyclopropyl-1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid
—— 6-(thiophen-2-yl)-4-(trifluoromethyl)pyridin-2(1H)-one 22123-11-1 C10H6F3NOS
6-(thiophen-2-yl)-4-(trifluoromethyl)pyridin-2(1H)-one
—— 5-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine 1319067-64-5 C7H5F3N4
5-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine
—— 2-(Thiophen-2-yl)pyridin-4-amine 1020540-64-0 C9H8N2S
2-(Thiophen-2-yl)pyridin-4-amine
—— Cytidine, 2'-deoxy-5-fluoro- 10356-76-0 C9H12FN3O4
Cytidine, 2'-deoxy-5-fluoro-
—— [[amino-(2,5-dichloro-4,6-dimethylpyridin-3-yl)methylidene]amino] 3-nitro-4,5-bis(phenylmethoxy)benzoate 1229803-77-3 C29H24Cl2N4O6
[[amino-(2,5-dichloro-4,6-dimethylpyridin-3-yl)methylidene]amino] 3-nitro-4,5-bis(phenylmethoxy)benzoate
—— 2-fluoro-4-methoxy-1-(trifluoromethyl)benzene 1214344-33-8 C8H6F4O
2-fluoro-4-methoxy-1-(trifluoromethyl)benzene
—— 3-iodo-1-(phenylsulfonyl)-1H-indole-7-carbonitrile 96631-87-7 C15H9IN2O2S
3-iodo-1-(phenylsulfonyl)-1H-indole-7-carbonitrile
—— 5-Acetaminomethyl-4-amin-2-methoxy-pyrimidin 6965-09-9 C8H12N4O2
5-Acetaminomethyl-4-amin-2-methoxy-pyrimidin
—— ethyl 3-amino-7-bromo-1,6-naphthyridine-2-carboxylate 1620239-76-0 C11H10BrN3O2
ethyl 3-amino-7-bromo-1,6-naphthyridine-2-carboxylate
—— 8-Bromo-9-pentofuranosyl-9H-purine-2,6-diol 686300-33-4 C10H11BrN4O6
8-Bromo-9-pentofuranosyl-9H-purine-2,6-diol
—— 1,2-Di-<s-triazolo<4,3-a>pyrid-3-yl>-ethan 4930-93-2 C14H12N6
1,2-Di-<s-triazolo<4,3-a>pyrid-3-yl>-ethan
—— 3-Amino-6-nitro-4-phenyl-2(1H)-chinolinon 36020-93-6 C15H11N3O3
3-Amino-6-nitro-4-phenyl-2(1H)-chinolinon
—— (-)-Tabernemontanine 2134-98-7 C21H26N2O3
(-)-Tabernemontanine