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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
—— Pyrimidin-4-ylamine trihydrochloride 174500-31-3 C4H8Cl3N3
Pyrimidin-4-ylamine trihydrochloride
—— 7β-amino-7α-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,diphenylmethyl ester 56610-72-1 C24H24N6O4S2
7β-amino-7α-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,diphenylmethyl ester
—— {[(Z)-(1-Cyano-2-ethoxy-2-oxoethylidene)amino]oxy}-N,N-dimethyl(morpholin-4-yl)methaniminium hexafluorophosphate 1075198-30-9 C12H19F6N4O4P
{[(Z)-(1-Cyano-2-ethoxy-2-oxoethylidene)amino]oxy}-N,N-dimethyl(morpholin-4-yl)methaniminium hexafluorophosphate
—— Intermediate of Clarithromycin 119665-62-2 C49H96N2O14Si2
Intermediate of Clarithromycin
—— tert-Butyl spiro[indoline-2,3'-pyrrolidine]-1'-carboxylate 1255574-67-4 C16H22N2O2
tert-Butyl spiro[indoline-2,3'-pyrrolidine]-1'-carboxylate
—— 5-Bromo-2-isobutylthiopyrimidine 1242336-74-8 C8H11BrN2S
5-Bromo-2-isobutylthiopyrimidine
—— 6,8-Dimethylquinoline hydrochloride 1255574-45-8 C11H12ClN
6,8-Dimethylquinoline hydrochloride
—— N,N-Dimethyl-1-(pyrrolidin-3-yl)methanamine hydrochloride 208711-42-6 C7H17ClN2
N,N-Dimethyl-1-(pyrrolidin-3-yl)methanamine hydrochloride
—— GlcNPhth[36Bn,4Ac]-beta-MP 140615-77-6 C37H35NO9
GlcNPhth[36Bn,4Ac]-beta-MP
—— Iridium(3+) tris(2-(isoquinolin-1-yl)benzen-1-ide) 435293-93-9 C45H30IrN3
Iridium(3+) tris(2-(isoquinolin-1-yl)benzen-1-ide)
—— N-((6-Chloropyridazin-3-yl)methyl)cyclopropanamine 1289386-54-4 C8H10ClN3
N-((6-Chloropyridazin-3-yl)methyl)cyclopropanamine
—— 7-[2-(3,3-Difluoro-4-phenoxybut-1-EN-1-YL)-3,5-dihydroxycyclopentyl]hept-5-enoic acid 209860-88-8 C22H28F2O5
7-[2-(3,3-Difluoro-4-phenoxybut-1-EN-1-YL)-3,5-dihydroxycyclopentyl]hept-5-enoic acid
—— 5-Amino-2-(dibenzylamino)-1,6-diphenylhex-4-en-3-one 156732-13-7 C32H32N2O
5-Amino-2-(dibenzylamino)-1,6-diphenylhex-4-en-3-one
—— S-1,3-Benzothiazol-2-yl (2-amino-1,3-thiazol-4-yl)[(triphenylmethoxy)imino]ethanethioate 143183-03-3 C31H22N4O2S3
S-1,3-Benzothiazol-2-yl (2-amino-1,3-thiazol-4-yl)[(triphenylmethoxy)imino]ethanethioate
—— (S)-1-(3-(2-(7-Chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)-phenyl)propanol 142569-70-8 C29H28ClNO2
(S)-1-(3-(2-(7-Chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)-phenyl)propanol
—— 7-Bromoquinolin-3-amine dihydrochloride 1266226-05-4 C9H9BrCl2N2
7-Bromoquinolin-3-amine dihydrochloride
—— 3-(2-Aminopyridin-3-YL)prop-2-enoic acid 773131-96-7 C8H8N2O2
3-(2-Aminopyridin-3-YL)prop-2-enoic acid
—— 1-(Oxan-2-yl)-3-[2-(pyridin-2-yl)ethenyl]-1H-indazol-6-amine 886230-76-8 C19H20N4O
1-(Oxan-2-yl)-3-[2-(pyridin-2-yl)ethenyl]-1H-indazol-6-amine
—— 5-(4-Amino-5-fluoro-2-oxo-1(2H)-pyrimidinyl)-1,3-oxathiolane-2-carboxylic acid 5-methyl-2-(1-methylethyl)cyclohexyl ester 147126-75-8 C18H26FN3O4S
5-(4-Amino-5-fluoro-2-oxo-1(2H)-pyrimidinyl)-1,3-oxathiolane-2-carboxylic acid 5-methyl-2-(1-methylethyl)cyclohexyl ester
—— 4-Iodo-1H-indole hydrochloride 81038-38-2 C8H7ClIN
4-Iodo-1H-indole hydrochloride
—— Ethyl 3-(4-amino-5-bromopyridin-3-yl)acrylate 912760-87-3 C10H11BrN2O2
Ethyl 3-(4-amino-5-bromopyridin-3-yl)acrylate
—— Ethyl 2-(pyrrolidin-3-yloxy)benzoate hydrochloride 1220032-96-1 C13H18ClNO3
Ethyl 2-(pyrrolidin-3-yloxy)benzoate hydrochloride
—— 1,3-Dichloroisoquinolin-4-amine 912773-27-4 C9H6Cl2N2
1,3-Dichloroisoquinolin-4-amine
—— 4,6-dichloro-5-propylpyrimidine 63797-51-3 C7H8Cl2N2
4,6-dichloro-5-propylpyrimidine
—— 4-(5-Bromopyridin-3-yl)pyrimidin-2-amine 913322-73-3 C9H7BrN4
4-(5-Bromopyridin-3-yl)pyrimidin-2-amine
—— 3-[4-Ethyl-2-(hydroxyimino)-5-nitrohex-3-en-1-yl]pyridine-2-carboxamide 162626-99-5 C14H18N4O4
3-[4-Ethyl-2-(hydroxyimino)-5-nitrohex-3-en-1-yl]pyridine-2-carboxamide
—— 1-(3-Phenylprop-2-enyl)piperazine hydrochloride 163596-56-3 C13H18N2*ClH
1-(3-Phenylprop-2-enyl)piperazine hydrochloride
—— Methanesulfonic acid--2-{[2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-2,3-dihydro-1H-1,2,4-triazole (1/1) 86386-77-8 C12H15F2N3O4S
Methanesulfonic acid--2-{[2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-2,3-dihydro-1H-1,2,4-triazole (1/1)
—— 3a,7a-Dihydroxy-5a-cholanate 15357-34-3 C24H40O4
3a,7a-Dihydroxy-5a-cholanate
—— 3-Bromo-6-chloro-2-iodopyridine 1211529-01-9 C5H2BrClIN
3-Bromo-6-chloro-2-iodopyridine
—— 7-Methoxy-2-methylimidazo[1,2-a]pyridine-3-carboxylic acid 854515-83-6 C10H10N2O3
7-Methoxy-2-methylimidazo[1,2-a]pyridine-3-carboxylic acid
—— (2R)-2-Amino-4-(7-hydroxy-2-oxo-2H-1-benzopyran-4-yl)butanoic acid 905442-42-4 C13H13NO5
(2R)-2-Amino-4-(7-hydroxy-2-oxo-2H-1-benzopyran-4-yl)butanoic acid
—— (5-amino-1,2,4-thiadiazol-3-yl)(ethoxyimino)ethanoic acid 75028-24-9 C6H8N4O3S
(5-amino-1,2,4-thiadiazol-3-yl)(ethoxyimino)ethanoic acid
—— 4,6-Dichloro-2-quinolinecarboxylic acid 902742-67-0 C10H5Cl2NO2
4,6-Dichloro-2-quinolinecarboxylic acid
—— 2-chloro-5H,6H,7H,8H-pyrido[3,4-d]pyrimidine 1196153-06-6 C7H8ClN3
2-chloro-5H,6H,7H,8H-pyrido[3,4-d]pyrimidine
—— [(6E,10E)-9-acetyloxy-6,10-dimethyl-3-methylidene-2-oxo-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-4-yl] (E)-4-hydroxy-2-(hydroxymethyl)but-2-enoate 38458-58-1 C22H28O8
[(6E,10E)-9-acetyloxy-6,10-dimethyl-3-methylidene-2-oxo-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-4-yl] (E)-4-hydroxy-2-(hydroxymethyl)but-2-enoate
—— Tetrabromophthalic acid, sodium salt 25357-79-3 C8H2Br4NaO4+
Tetrabromophthalic acid, sodium salt
—— 1, N-(2-chloroethyl)-N'-(6-chloro-2-methoxy-9-acridinyl)-, dihydrochloride 17070-45-0 C19H22Cl3N3O
1, N-(2-chloroethyl)-N'-(6-chloro-2-methoxy-9-acridinyl)-, dihydrochloride
—— N,N''-bis[[(4-chlorophenyl)amino]iminomethyl]piperazine-1,4-dicarboxamidine dihydrochloride 19803-62-4 C20H24Cl2N10*(x)ClH
N,N''-bis[[(4-chlorophenyl)amino]iminomethyl]piperazine-1,4-dicarboxamidine dihydrochloride
—— Demeclocycline 127-33-3 C21H21ClN2O8
Demeclocycline
—— Carbostyril, monosodium salt 4510-76-3 C9H7NNaO2+
Carbostyril, monosodium salt
—— 2-(3-(Pyrimidin-2-yl)phenyl)ethylamine 910404-93-2 C12H13N3
2-(3-(Pyrimidin-2-yl)phenyl)ethylamine
—— 5-chloro-2-(piperidin-4-yl)pyrimidine 944903-10-0 C9H12ClN3
5-chloro-2-(piperidin-4-yl)pyrimidine
—— (4-chloropyrimidin-2-yl)methanol 1093880-89-7 C5H5ClN2O
(4-chloropyrimidin-2-yl)methanol
—— trans-1-cinnamylpiperazine dihydrochloride 163596-56-3 C13H18N2*2ClH
trans-1-cinnamylpiperazine dihydrochloride
—— 4-Nitrophenyl 2-(furfurylsulfinyl)acetic acid 123855-55-0 C13H11NO6S
4-Nitrophenyl 2-(furfurylsulfinyl)acetic acid
—— 6-Bromo-5-fluoroquinoline hydrochloride 127827-51-4 C9H6BrClFN
6-Bromo-5-fluoroquinoline hydrochloride
—— (3aR,4R,5R,6aS)-2-Oxo-4-{3-oxo-4-[3-(trifluoromethyl)phenoxy]but-1-en-1-yl}hexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate 54142-64-2 C31H25F3O6
(3aR,4R,5R,6aS)-2-Oxo-4-{3-oxo-4-[3-(trifluoromethyl)phenoxy]but-1-en-1-yl}hexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate
—— Cinchonidine sulphate 524-61-8 C38H46N4O6S
Cinchonidine sulphate
—— 4-Amino-N-methoxy-N-methyl-2-(methylthio)pyrimidine-5-carboxamide 741714-02-3 C8H12N4O2S
4-Amino-N-methoxy-N-methyl-2-(methylthio)pyrimidine-5-carboxamide