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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
—— 2,2,2-Trifluoro-1-(4-methylpyridin-2-yl)ethanone 1060804-97-8 C8H6F3NO
2,2,2-Trifluoro-1-(4-methylpyridin-2-yl)ethanone
—— 6-(4-{(E)-2-[4-(Hexane-1-sulfonyl)-phenyl]-vinyl}-phenoxy)-hexan-1-ol 133261-44-6 C26H36O4S
6-(4-{(E)-2-[4-(Hexane-1-sulfonyl)-phenyl]-vinyl}-phenoxy)-hexan-1-ol
—— 6-O-Methyl-2',4''-bis-O-(trimethylsilyl)-9-[O-(1-ethoxy-1-methylethyl)oxime] Erythromycin 119665-62-2 C49H96N2O14Si2
6-O-Methyl-2',4''-bis-O-(trimethylsilyl)-9-[O-(1-ethoxy-1-methylethyl)oxime] Erythromycin
—— 2,2-bis((S)-4-phenyl-4,5-dihydrooxazol-2-yl)acetonitrile 150639-33-1 C20H17N3O2
2,2-bis((S)-4-phenyl-4,5-dihydrooxazol-2-yl)acetonitrile
—— 3-aminoisoquinoline-6-carboxylic acid 1337880-79-1 C10H8N2O2
3-aminoisoquinoline-6-carboxylic acid
—— 4-hydrazino-2-(trifluoromethyl)pyridine 1228535-68-9 C6H6F3N3
4-hydrazino-2-(trifluoromethyl)pyridine
—— 6-chloro-4-methoxyquinolin-2-(1H)-one 865817-83-0 C10H8ClNO2
6-chloro-4-methoxyquinolin-2-(1H)-one
—— 5-Bromo-4-chloro-3-indolyl phosphate disodium salt 1.5-hydrate 102185-33-1 C8H6BrClNNaO4P
5-Bromo-4-chloro-3-indolyl phosphate disodium salt 1.5-hydrate
—— 2,6-Pyridinedicarboxylic acid, sodium salt (1:2) 17956-40-0 C7H5NNaO4
2,6-Pyridinedicarboxylic acid, sodium salt (1:2)
—— 1-chloro-3,5-di-(4-chlorobenzoyl)-2-deoxy-α-D-ribose 21740-23-8 C19H15Cl3O5
1-chloro-3,5-di-(4-chlorobenzoyl)-2-deoxy-α-D-ribose
—— [(2R,3R,5S)-5-chloro-3-(4-chlorobenzoyl)oxyoxolan-2-yl]methyl 4-chlorobenzoate 21740-23-8 C19H15Cl3O5
[(2R,3R,5S)-5-chloro-3-(4-chlorobenzoyl)oxyoxolan-2-yl]methyl 4-chlorobenzoate
—— (2-Morpholinopyrimidin-5-yl)methanol 937796-13-9 C9H13N3O2
(2-Morpholinopyrimidin-5-yl)methanol
—— Sulfameter sodium 18179-67-4 C11H11N4NaO3S
Sulfameter sodium
—— 2-Amino-6-bromoquinoline hydrochloride 1170935-81-5 C9H8BrClN2
2-Amino-6-bromoquinoline hydrochloride
—— (+)-Bicuculline methochloride 53552-05-9 C21H20ClNO6
(+)-Bicuculline methochloride
—— 4-(3-hydroxypropylamino)-1,3-dimethyl-4H-pyrimidin-2-one 34654-80-3 C9H17N3O2
4-(3-hydroxypropylamino)-1,3-dimethyl-4H-pyrimidin-2-one
—— Tetrasodium 4-(3-(3-carboxylato-5-hydroxy-1-(4-sulphonatophenyl)-1H-pyrazol-4-yl)allylidene)-4,5-dihydro-5-oxo-1-(4-sulphonatophenyl)-1H-pyrazole-3-carboxylate 70024-44-1 C23H12N4Na4O12S2
Tetrasodium 4-(3-(3-carboxylato-5-hydroxy-1-(4-sulphonatophenyl)-1H-pyrazol-4-yl)allylidene)-4,5-dihydro-5-oxo-1-(4-sulphonatophenyl)-1H-pyrazole-3-carboxylate
—— Diethylethoxyammonium chloride 13989-32-7 C6H15ClNO-
Diethylethoxyammonium chloride
—— (5-Ethenyl-1-azabicyclo[2.2.2]octan-2-yl)-(6-methoxyquinolin-4-yl)methanamine 168960-95-0 C20H25N3O
(5-Ethenyl-1-azabicyclo[2.2.2]octan-2-yl)-(6-methoxyquinolin-4-yl)methanamine
—— 2-Amino-5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazol-4(5H)-one 329249-53-8 C18H20N4O2S
2-Amino-5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazol-4(5H)-one
—— (R)-[(4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-quinolin-4-ylmethanol;dihydrochloride 24302-67-8 C19H24Cl2N2O
(R)-[(4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-quinolin-4-ylmethanol;dihydrochloride
—— [(2S,3S,4R,5S,6S)-3,4-diacetyloxy-6-phenylsulfanyl-5-(2,2,2-trichloroethoxycarbonylamino)oxan-2-yl]methyl acetate 187022-49-7 C21H24Cl3NO9S
[(2S,3S,4R,5S,6S)-3,4-diacetyloxy-6-phenylsulfanyl-5-(2,2,2-trichloroethoxycarbonylamino)oxan-2-yl]methyl acetate
—— (+)-Camphor Bromide 10293-06-8 C10H15BrO
(+)-Camphor Bromide
—— (R)-[(2R,4S,5R)-1-benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl]-quinolin-4-ylmethanol;chloride 69257-04-1 C26H29ClN2O
(R)-[(2R,4S,5R)-1-benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl]-quinolin-4-ylmethanol;chloride
—— 6-Bromo-4,4-dimethyl-1,2,3,4-tetrahydroquinoline hydrochloride 135631-91-3 C11H15BrClN
6-Bromo-4,4-dimethyl-1,2,3,4-tetrahydroquinoline hydrochloride
—— 2(1H)-Pyridinethione, 1-hydroxy-, sodium salt (1:1) 15922-78-8 C5H5NNaOS
2(1H)-Pyridinethione, 1-hydroxy-, sodium salt (1:1)
—— (3R,4S)-1-(tert-Butoxycarbonyl)-4-(ethoxycarbonyl)pyrrolidine-3-carboxylic acid 252919-44-1 C13H21NO6
(3R,4S)-1-(tert-Butoxycarbonyl)-4-(ethoxycarbonyl)pyrrolidine-3-carboxylic acid
—— Methyl[1-(piperidin-4-yl)pyridin-4(1H)-ylidene]oxidanium chloride 84145-43-7 C11H17ClN2O
Methyl[1-(piperidin-4-yl)pyridin-4(1H)-ylidene]oxidanium chloride
—— N-(2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl)-N-(pyridin-2-yl)cyclohexanecarboxamide hydrochloride 146714-97-8 C25H35ClN4O2
N-(2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl)-N-(pyridin-2-yl)cyclohexanecarboxamide hydrochloride
—— (2R,4aS,6S,6aS,9aR)-7-Benzyl-2-phenyl-6-(phenylsulfanyl)hexahydro-2H-[1,3]dioxino[4',5':5,6]pyrano[3,4-d][1,3]oxazol-8(6H)-one 910805-49-1 C27H25NO5S
(2R,4aS,6S,6aS,9aR)-7-Benzyl-2-phenyl-6-(phenylsulfanyl)hexahydro-2H-[1,3]dioxino[4',5':5,6]pyrano[3,4-d][1,3]oxazol-8(6H)-one
—— (4R,6R,8S,9S,13R)-8-acetyl-6,9,13-trimethyl-6-phenyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one 24356-94-3 C29H36O4
(4R,6R,8S,9S,13R)-8-acetyl-6,9,13-trimethyl-6-phenyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one
—— 4,6-O-Benzylidene-D-threo-hexopyranose 97232-16-1 C13H16O6
4,6-O-Benzylidene-D-threo-hexopyranose
—— tert-butyl (2R)-2-(aminomethyl)pyrrolidine-1-carboxylate hydrochloride 1190890-12-0 C10H20N2O2*ClH
tert-butyl (2R)-2-(aminomethyl)pyrrolidine-1-carboxylate hydrochloride
—— (2S,4R)-Methyl 4-(((benzyloxy)carbonyl)amino)pyrrolidine-2-carboxylate hydrochloride 1217626-26-0 C14H19ClN2O4
(2S,4R)-Methyl 4-(((benzyloxy)carbonyl)amino)pyrrolidine-2-carboxylate hydrochloride
—— 5-Propyl-2-pyrimidinamine 39268-72-9 C7H11N3
5-Propyl-2-pyrimidinamine
—— (3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(4S,6S)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-10-hydroxyimino-4-[(4R,5R,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one 13127-18-9 C37H68N2O13
(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(4S,6S)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-10-hydroxyimino-4-[(4R,5R,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one
—— [(4R)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl 4-methylbenzenesulfonate 134071-44-6 C21H20Cl2N2O5S
[(4R)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl 4-methylbenzenesulfonate
—— 4-[2-hydroxy-1-[(Z)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoic acid 88430-50-6 C24H30O5
4-[2-hydroxy-1-[(Z)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoic acid
—— 7,8-dihydroquinazolin-6(5H)-one 944895-73-2 C8H8N2O
7,8-dihydroquinazolin-6(5H)-one
—— 5-chloro-6-quinolinecarbaldehyde 180421-64-1 C10H6ClNO
5-chloro-6-quinolinecarbaldehyde
—— 3-amino-1H-pyrazolo[3,4-b]pyridin-7-ium-7-olate 1198475-27-2 C6H6N4O
3-amino-1H-pyrazolo[3,4-b]pyridin-7-ium-7-olate
—— 4-Bromo-8-chloro-5-methoxyquinoline 1189107-37-6 C10H7BrClNO
4-Bromo-8-chloro-5-methoxyquinoline
—— 4,7-Dibromo-6-methylquinoline 1189107-21-8 C10H7Br2N
4,7-Dibromo-6-methylquinoline
—— 4,6-Dibromo-2,8-dimethylquinoline 1189107-47-8 C11H9Br2N
4,6-Dibromo-2,8-dimethylquinoline
—— 4-Bromo-5,8-difluoroquinoline 1189106-41-9 C9H4BrF2N
4-Bromo-5,8-difluoroquinoline
—— 4,8-Dibromo-2-phenylquinoline 1189106-08-8 C15H9Br2N
4,8-Dibromo-2-phenylquinoline
—— 4,8-Dibromo-6-methylquinoline 1189106-63-5 C10H7Br2N
4,8-Dibromo-6-methylquinoline
—— 4,6-Dibromo-7-methylquinoline 1189105-55-2 C10H7Br2N
4,6-Dibromo-7-methylquinoline
—— 3-Bromo-6-fluoro-4-hydroxyquinoline 1065087-77-5 C9H5BrFNO
3-Bromo-6-fluoro-4-hydroxyquinoline
—— 4,8-Dibromo-2,6-dimethylquinoline 1189107-53-6 C11H9Br2N
4,8-Dibromo-2,6-dimethylquinoline