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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
—— 6-bromo-[1,2,3]triazolo[1,5-a]pyridine 192642-82-3 C6H4BrN3
6-bromo-[1,2,3]triazolo[1,5-a]pyridine
—— (2R,4R)-(+)-<2-(bromomethyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl>methyl benzoate 61397-56-6 C18H15BrCl2O4
(2R,4R)-(+)-<2-(bromomethyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl>methyl benzoate
—— germacranolide eucannabinolide 38458-58-1 C22H28O8
germacranolide eucannabinolide
—— 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine dihydrochloride 157327-44-1 C6H9N3*2ClH
4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine dihydrochloride
—— 6-bromo-1,4-dihydro-2H-isoquinolin-3-one 943749-57-3 C9H8BrNO
6-bromo-1,4-dihydro-2H-isoquinolin-3-one
—— 5-bromo-4-methyl-2-(trifluoromethyl)pyrimidine 1100767-04-1 C6H4BrF3N2
5-bromo-4-methyl-2-(trifluoromethyl)pyrimidine
—— N,N-diphenyl pyridin-4-amine 69663-19-0 C17H14N2
N,N-diphenyl pyridin-4-amine
—— tert-butyl 3,3-dimethyl-5-oxopiperidine-1-carboxylate 1000894-83-6 C12H21NO3
tert-butyl 3,3-dimethyl-5-oxopiperidine-1-carboxylate
—— 1,4-dimethyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonyl chloride 841275-84-1 C10H9ClN2O4S
1,4-dimethyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonyl chloride
—— 2-(4-bromo-3-fluorophenyl)pyrrolidine 1175528-91-2 C10H11BrFN
2-(4-bromo-3-fluorophenyl)pyrrolidine
—— 3-hydroxy-3-(2-(naphthalen-2-yl)-2-oxoethyl)indolin-2-one 6765-52-2 C20H15NO3
3-hydroxy-3-(2-(naphthalen-2-yl)-2-oxoethyl)indolin-2-one
—— (6-nitropyridin-3-yl)boronic acid 1236354-21-4 C5H5BN2O4
(6-nitropyridin-3-yl)boronic acid
—— tert-butyl (S)-(1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamate 1620056-47-4 C18H18Br2F2N2O2
tert-butyl (S)-(1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamate
—— 2-(3-Aminophenyl)butanoic acid 21762-24-3 C10H13NO2
2-(3-Aminophenyl)butanoic acid
—— 1,2,3,3a,4,8b-hexahydrocyclopenta[b]indole 80278-94-0 C11H13N
1,2,3,3a,4,8b-hexahydrocyclopenta[b]indole
—— ethyl 5-bromo-2-oxopentanoate 57224-29-0 C7H11BrO3
ethyl 5-bromo-2-oxopentanoate
—— (cyclohexanone yl-3) acatate de methyle 2808-12-0 C9H14O3
(cyclohexanone yl-3) acatate de methyle
—— 4,6-dichloro-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidine 21254-22-8 C8H8Cl2N4
4,6-dichloro-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidine
—— 6-Methylen-androst-4-en-3,17-dion 19457-55-7 C20H26O2
6-Methylen-androst-4-en-3,17-dion
—— 5-(methoxycarbonyl)-3-methyl-2-pyridone 66909-31-7 C8H9NO3
5-(methoxycarbonyl)-3-methyl-2-pyridone
—— (2R,3S)-3-amino-1-[benzyl(2-methylpropyl)amino]-4-phenylbutan-2-ol 1213710-50-9 C21H30N2O
(2R,3S)-3-amino-1-[benzyl(2-methylpropyl)amino]-4-phenylbutan-2-ol
—— 8-epi-15-J2-IsoP 60203-57-8 C20H30O4
8-epi-15-J2-IsoP
—— 9-deoxa-9,10-dehydroprostaglandin D<sub>2</sub> 60203-57-8 C20H30O4
9-deoxa-9,10-dehydroprostaglandin D<sub>2</sub>
—— 3-phenyl-2-(triethylsilyl)-1H-indole 1504-16-1 C20H25NSi
3-phenyl-2-(triethylsilyl)-1H-indole
—— (6S)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxylic acid 1375541-21-1 C15H11N3O3
(6S)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxylic acid
—— 2-bromothiophene-3-carboxamide 189330-06-1 C5H4BrNOS
2-bromothiophene-3-carboxamide
—— 3-ethynyl-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide 957147-18-1 C23H24F3N3O
3-ethynyl-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide
—— (3S,4S,5R)-6-allyloxy-3,4,5-tris-benzyloxy-2,2-bis(4-methoxybenzyloxymethyl)tetrahydropyrane 1210344-28-7 C47H52O9
(3S,4S,5R)-6-allyloxy-3,4,5-tris-benzyloxy-2,2-bis(4-methoxybenzyloxymethyl)tetrahydropyrane
—— ((2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)methyl-1,3-dioxolan-4-yl)methyl 4-methylbenzenesulfonate 134071-44-6 C21H20Cl2N2O5S
((2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)methyl-1,3-dioxolan-4-yl)methyl 4-methylbenzenesulfonate
—— 1-benzyl-4-(2-methoxyphenyl)-1,2,3,6-tetrahydro-pyridine 113411-59-9 C19H21NO
1-benzyl-4-(2-methoxyphenyl)-1,2,3,6-tetrahydro-pyridine
—— 6-nitro-1',3',3'-trimethylspiro(2H-1-benzothiopyran-2,2'-indoline) 85000-11-9 C19H18N2O2S
6-nitro-1',3',3'-trimethylspiro(2H-1-benzothiopyran-2,2'-indoline)
—— olean-12-en-3β-ol 559-70-6 C30H50O
olean-12-en-3β-ol
—— β-amyrin 559-70-6 C30H50O
β-amyrin
—— (5β)-olean-12-en-3β-ol 559-70-6 C30H50O
(5β)-olean-12-en-3β-ol
—— olean-12-ene-3-ol 559-70-6 C30H50O
olean-12-ene-3-ol
—— (14β)-olean-12-en-3β-ol 559-70-6 C30H50O
(14β)-olean-12-en-3β-ol
—— olean-12-en-3α-ol 559-70-6 C30H50O
olean-12-en-3α-ol
—— 3,4-O-isopropylidene-3(R),4(S)-dihydroxycyclohexanone 121573-17-9 C9H14O3
3,4-O-isopropylidene-3(R),4(S)-dihydroxycyclohexanone
—— (3'R)-3-bromo-1,3'-bipyrrolidin-2-one 1217259-67-0 C8H13BrN2O
(3'R)-3-bromo-1,3'-bipyrrolidin-2-one
—— (4S)-[<sup>2</sup>H]NADPH 74784-45-5 C21H30N7O17P3
(4S)-[<sup>2</sup>H]NADPH
—— 5-Chloro-7-pyridin-4-yl-1,6-naphthyridine 1211595-82-2 C13H8ClN3
5-Chloro-7-pyridin-4-yl-1,6-naphthyridine
—— 4-(4-bromo-3-(bromomethyl)phenoxy)furo[3,2-c]pyridine 1609581-25-0 C14H9Br2NO2
4-(4-bromo-3-(bromomethyl)phenoxy)furo[3,2-c]pyridine
—— (5-fluoro-6-methoxypyridin-3-yl)methanol 959616-65-0 C7H8FNO2
(5-fluoro-6-methoxypyridin-3-yl)methanol
—— 8-bromo-6-chloro-[1,2,4]triazolo[1,5-a]pyridine 1433822-19-5 C6H3BrClN3
8-bromo-6-chloro-[1,2,4]triazolo[1,5-a]pyridine
—— 1-(tert-butyl)-3-((5-chloro-3-(chloromethyl)pyridin-2-yl)methyl)-1H-pyrrolo[2,3-b]pyridin-2(3H)-one 1455358-12-9 C18H19Cl2N3O
1-(tert-butyl)-3-((5-chloro-3-(chloromethyl)pyridin-2-yl)methyl)-1H-pyrrolo[2,3-b]pyridin-2(3H)-one
—— 1-(tert-butyl)-3-((5-chloro-3-(hydroxymethyl)pyridin-2-yl)methyl)-1H-pyrrolo[2,3-b]pyridin-2(3H)-one 1455358-11-8 C18H20ClN3O2
1-(tert-butyl)-3-((5-chloro-3-(hydroxymethyl)pyridin-2-yl)methyl)-1H-pyrrolo[2,3-b]pyridin-2(3H)-one
—— Methyl 1,2,5-thiadiazole-3-carboxylate 63875-20-7 C4H4N2O2S
Methyl 1,2,5-thiadiazole-3-carboxylate
—— 7-bromo-2-methyl-3,4-dihydroisoquinolin-1(2H)-one 1313399-68-6 C10H10BrNO
7-bromo-2-methyl-3,4-dihydroisoquinolin-1(2H)-one
—— spiro[2.5]octane-6-carbaldehyde 849671-57-4 C9H14O
spiro[2.5]octane-6-carbaldehyde
—— 5H-imidazo[1,2-b]pyrazole 251-80-9 C5H5N3
5H-imidazo[1,2-b]pyrazole