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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
—— 1,1,2,3-tetramethyl-1H-benzo[e]indol-3-ium 58464-25-8 C16H18N
1,1,2,3-tetramethyl-1H-benzo[e]indol-3-ium
—— cis-Ethyl 3-aminocyclobutanecarboxylate hydrochloride 957793-35-0 C7H13NO2*ClH
cis-Ethyl 3-aminocyclobutanecarboxylate hydrochloride
—— tabernaemontanine 2134-98-7 C21H26N2O3
tabernaemontanine
—— 8-Chloro-2-methylquinoline-4-carboxylic acid 52413-67-9 C11H8ClNO2
8-Chloro-2-methylquinoline-4-carboxylic acid
—— 4,6-Diamino-2-chlor-pyrimidin 53557-61-2 C4H5ClN4
4,6-Diamino-2-chlor-pyrimidin
—— 6-methoxypyridine-2,3-diamine dihydrochloride 94166-62-8 C6H9N3O*2ClH
6-methoxypyridine-2,3-diamine dihydrochloride
—— 3,3-Difluorocyclohexane-1-carbonitrile 1227808-14-1 C7H9F2N
3,3-Difluorocyclohexane-1-carbonitrile
—— 4-aminopiperidine-1,4-dicarboxylic acid-1-tert-butyl ester-4-ethyl ester 1187321-32-9 C13H24N2O4
4-aminopiperidine-1,4-dicarboxylic acid-1-tert-butyl ester-4-ethyl ester
—— Δ<sup>3,5</sup>-Androstadien-3,17-dion 1420-49-1 C19H24O2
Δ<sup>3,5</sup>-Androstadien-3,17-dion
—— 3-(2-bromo-1-hydroxyethyl)-10,11-dihydro-5H-dibenzo[c,g]chromen-8(9H)-one 1378391-38-8 C19H17BrO3
3-(2-bromo-1-hydroxyethyl)-10,11-dihydro-5H-dibenzo[c,g]chromen-8(9H)-one
—— 5-Sulfoquinolin-8-olate 84-88-8 C9H6NO4S
5-Sulfoquinolin-8-olate
—— Morellin 1183-12-6 C33H36O7
Morellin
—— 4-((1RS,2RS,3aSR,8bSR)-2-hydroxy-1-((3SR,E)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)-2 ,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-5-yl)butanoic acid 88430-50-6 C24H30O5
4-((1RS,2RS,3aSR,8bSR)-2-hydroxy-1-((3SR,E)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)-2 ,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-5-yl)butanoic acid
—— D-(+)-3-Bromocamphor 10293-06-8 C10H15BrO
D-(+)-3-Bromocamphor
—— 2-(5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-5-(phenylazo)pyrimidine-4,6-diamine 1350653-29-0 C23H17F2N9
2-(5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-5-(phenylazo)pyrimidine-4,6-diamine
—— N-(3-(7-amino-1-methyl-2-oxo-1,4-dihydropyrimido[4,5-d]-pyrimidin-3(2H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide 839708-29-1 C22H19F3N6O2
N-(3-(7-amino-1-methyl-2-oxo-1,4-dihydropyrimido[4,5-d]-pyrimidin-3(2H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide
—— methyl (2S,3S)-2-(tert-butoxycarbonyl)amino-3-hydroxy-3-phenylpropionate 17193-36-1 C15H21NO5
methyl (2S,3S)-2-(tert-butoxycarbonyl)amino-3-hydroxy-3-phenylpropionate
—— tert-butyl (R)-(1-(1H-indol-3-yl)propan-2-yl)carbamate 847199-90-0 C16H22N2O2
tert-butyl (R)-(1-(1H-indol-3-yl)propan-2-yl)carbamate
—— 18-(2-Carboxyethyl)-20-(carboxymethyl)-12-ethenyl-7-ethyl-3,8,13,17-tetramethyl-17,18,22,23-tetrahydroporphyrin-2-carboxylic acid 19660-77-6 C34H36N4O6
18-(2-Carboxyethyl)-20-(carboxymethyl)-12-ethenyl-7-ethyl-3,8,13,17-tetramethyl-17,18,22,23-tetrahydroporphyrin-2-carboxylic acid
—— Isomorellin 1183-12-6 C33H36O7
Isomorellin
—— propylamino-4 bromo-7 quinoleine 71595-18-1 C12H13BrN2
propylamino-4 bromo-7 quinoleine
—— 5,5-difluoro-1,3,2-dioxathiane 2,2-dioxide 1215071-15-0 C3H4F2O4S
5,5-difluoro-1,3,2-dioxathiane 2,2-dioxide
—— ethyl 4-(benzofuran-2-yl)-2,4-dioxobutanoate 106276-58-8 C14H12O5
ethyl 4-(benzofuran-2-yl)-2,4-dioxobutanoate
—— tert-butyl 4-hydroxy-1H-indazole-1-carboxylate 1228874-81-4 C12H14N2O3
tert-butyl 4-hydroxy-1H-indazole-1-carboxylate
—— Chlorin e6 19660-77-6 C34H36N4O6
Chlorin e6
—— tert-butyl 4-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-7-yl)piperidine-1-carboxylate 717900-74-8 C16H21ClN4O2
tert-butyl 4-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-7-yl)piperidine-1-carboxylate
—— 3-(2-carboxy-ethyl)-5-sulfomethyl-1H-indole-2-carboxylic acid ethyl ester 771466-66-1 C15H17NO7S
3-(2-carboxy-ethyl)-5-sulfomethyl-1H-indole-2-carboxylic acid ethyl ester
—— 1-Methoxy-3-indolylmethyl glucosinolate 5187-84-8 C17H22N2O10S2
1-Methoxy-3-indolylmethyl glucosinolate
—— 5-bromopyrazolo[1,5-a]pyridine-3-carbonitrile 1352900-95-8 C8H4BrN3
5-bromopyrazolo[1,5-a]pyridine-3-carbonitrile
—— N-phenyl-4-(5-phenylthiophen-2-yl)aniline 1085434-10-1 C22H17NS
N-phenyl-4-(5-phenylthiophen-2-yl)aniline
—— bicyclo[4.1.0]heptane-3-carboxylic acid 710314-32-2 C8H12O2
bicyclo[4.1.0]heptane-3-carboxylic acid
—— tert-butyl 4-(2,6-dichloropyridin-4-yl)-5 ,6-dihydropyridine-1(2H)-carboxylate 1239363-36-0 C15H18Cl2N2O2
tert-butyl 4-(2,6-dichloropyridin-4-yl)-5 ,6-dihydropyridine-1(2H)-carboxylate
—— 4-(1H-1,2,3-triazol-1-yl)benzoic acid 216959-87-4 C9H7N3O2
4-(1H-1,2,3-triazol-1-yl)benzoic acid
—— 1-butyl-2-methylbenzo[cd]indol-1-ium iodide 1151666-46-4 C16H18N*I
1-butyl-2-methylbenzo[cd]indol-1-ium iodide
—— Flunisolide, >=97% 77326-96-6 C24H31FO6
Flunisolide, >=97%
—— (1R,3S)-3-trifluoromethylcyclohexylamine hydrochloride 1529782-04-4 C7H12F3N*ClH
(1R,3S)-3-trifluoromethylcyclohexylamine hydrochloride
—— ethyl (E)-4,4,4-trifluoro-3-(methylamino)but-2-enoate 121303-76-2 C7H10F3NO2
ethyl (E)-4,4,4-trifluoro-3-(methylamino)but-2-enoate
—— 16β-formyloxy-3β-(<i>O</i><sup>4</sup>β-D-glucopyranosyl-<i>O</i><sup>3</sup>-methyl-β-D-fucopyranosyloxy)-14-hydroxy-5β,14β-card-20(22)-enolide 6022-99-7 C37H56O15
16β-formyloxy-3β-(<i>O</i><sup>4</sup>β-D-glucopyranosyl-<i>O</i><sup>3</sup>-methyl-β-D-fucopyranosyloxy)-14-hydroxy-5β,14β-card-20(22)-enolide
—— 3-chloro-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazine 1270497-66-9 C12H18ClN3OSi
3-chloro-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazine
—— 6-Dehydro-19-nor-testosteron 6242-39-3 C18H24O2
6-Dehydro-19-nor-testosteron
—— 6'-Hydroxycinchonin 524-63-0 C19H22N2O2
6'-Hydroxycinchonin
—— tert-butyl 3-[(2-{[(2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]oct-2-yl]carbonyl}hydrazinyl)carbonyl]pyrrolidine-1-carboxylate 1452467-45-6 C24H33N5O6
tert-butyl 3-[(2-{[(2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]oct-2-yl]carbonyl}hydrazinyl)carbonyl]pyrrolidine-1-carboxylate
—— Caffeoyl-coenzyme A 53034-79-0 C30H42N7O19P3S
Caffeoyl-coenzyme A
—— 3H-Pyrazol-3-one, 4-((1,3-dihydro-1,3,3-trimethyl-2H-indol-2-ylidene)ethylidene)-2,4-dihydro-5-methyl-2-phenyl- 5190-63-6 C23H23N3O
3H-Pyrazol-3-one, 4-((1,3-dihydro-1,3,3-trimethyl-2H-indol-2-ylidene)ethylidene)-2,4-dihydro-5-methyl-2-phenyl-
—— 9-Ethylidene-3-oxatricyclo(6.2.1.02,7)undecane-4-one 69486-14-2 C12H16O2
9-Ethylidene-3-oxatricyclo(6.2.1.02,7)undecane-4-one
—— [(3aR,4R,6Z,9R,10Z,11aR)-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 64439-43-6 C22H28O8
[(3aR,4R,6Z,9R,10Z,11aR)-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
—— methyl 4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxylate 221316-61-6 C9H11NO2S
methyl 4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxylate
—— 5-(tert-butyl) 2-methyl 6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxylate 1135123-74-8 C14H19NO4S
5-(tert-butyl) 2-methyl 6,7-dihydrothieno[3,2-c]pyridine-2,5(4H)-dicarboxylate
—— Tiaprost 71116-82-0 C20H28O6S
Tiaprost
—— tert-butyl 7-nitro-3,4-dihydro-1,5-naphthyridine-1(2H)-carboxylate 1061148-41-1 C13H17N3O4
tert-butyl 7-nitro-3,4-dihydro-1,5-naphthyridine-1(2H)-carboxylate