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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
—— 1,2-bis(4-ethynylphenyl)-1,2-diphenylethene 1240785-42-5 C30H20
1,2-bis(4-ethynylphenyl)-1,2-diphenylethene
—— (7R,8aS)-tert-butyl 7-hydroxyhexahydropyrrolo[1,2-a]pyrazine-2(1H)-carboxylate 1204603-42-8 C12H22N2O3
(7R,8aS)-tert-butyl 7-hydroxyhexahydropyrrolo[1,2-a]pyrazine-2(1H)-carboxylate
—— (2-chloro-9-methyl-9H-purin-6-yl)-(4-chloro-phenyl)-amine 1062592-41-9 C12H9Cl2N5
(2-chloro-9-methyl-9H-purin-6-yl)-(4-chloro-phenyl)-amine
—— 2-(diisopropylsilyl)pyridine 1232692-92-0 C11H19NSi
2-(diisopropylsilyl)pyridine
—— 1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-pinacolatoboronaphthalene 853998-14-8 C20H31BO2
1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-pinacolatoboronaphthalene
—— tert-butyl (S)-4-(((tert-butyldimethylsilyl)oxy)methyl)-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide 1338090-89-3 C14H29NO6SSi
tert-butyl (S)-4-(((tert-butyldimethylsilyl)oxy)methyl)-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide
—— 5,7-difluoro-1,2,3,4-tetrahydroquinoline 939758-78-8 C9H9F2N
5,7-difluoro-1,2,3,4-tetrahydroquinoline
—— 6,6'-dimethoxy-2,2'-bipyridine 39858-88-3 C12H12N2O2
6,6'-dimethoxy-2,2'-bipyridine
—— 1-(6-chloro-2-pyridinyl)piperazine hydrochloride 95884-49-4 C9H12ClN3*ClH
1-(6-chloro-2-pyridinyl)piperazine hydrochloride
—— 3-chloro-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxylic acid 458543-79-8 C9H5Cl2N3O2
3-chloro-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxylic acid
—— 2-Piperidino-3-chloropyridine 282723-20-0 C10H13ClN2
2-Piperidino-3-chloropyridine
—— 4-methoxy-1-methyl-1H-pyrazole 15131-95-0 C5H8N2O
4-methoxy-1-methyl-1H-pyrazole
—— 3-bromopyrazolo[1,5-a]pyrazine 53902-93-5 C6H4BrN3
3-bromopyrazolo[1,5-a]pyrazine
—— (±)-trans-2-(aminomethyl)cyclopropanecarboxylic acid 36489-13-1 C5H9NO2
(±)-trans-2-(aminomethyl)cyclopropanecarboxylic acid
—— (1S,3R)-3-Methyl-cyclohexanol 24965-92-2 C7H14O
(1S,3R)-3-Methyl-cyclohexanol
—— methyl (2)-(1-methyl-2-pyrrolidinylidene)acetate 78167-68-7 C8H13NO2
methyl (2)-(1-methyl-2-pyrrolidinylidene)acetate
—— 6,6'-dibromoisoindigo 1147124-21-7 C16H8Br2N2O2
6,6'-dibromoisoindigo
—— 3,6-bis(thieno[3,2-b]thiophen-2-yl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione 1246679-11-7 C18H8N2O2S4
3,6-bis(thieno[3,2-b]thiophen-2-yl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione
—— methyl 5-((2,4-difluorobenzyl)carbamoyl)-1-(2,2-dimethoxyethyl)-3-methoxy-4-oxo-1,4-dihydropyridine-2-carboxylate 1616340-68-1 C20H22F2N2O7
methyl 5-((2,4-difluorobenzyl)carbamoyl)-1-(2,2-dimethoxyethyl)-3-methoxy-4-oxo-1,4-dihydropyridine-2-carboxylate
—— 4-Vinyl-4'-carboxy-diphenyl 92496-30-5 C15H12O2
4-Vinyl-4'-carboxy-diphenyl
—— 4,4,4-trifluoro-3-aminocrotonic acid ethyl ester 372-29-2 C6H8F3NO2
4,4,4-trifluoro-3-aminocrotonic acid ethyl ester
—— 2-methyldibenzothiophene 20928-02-3 C13H10S
2-methyldibenzothiophene
—— 1-propyl-3,4-dihydro-2H-pyridine 93101-22-5 C8H15N
1-propyl-3,4-dihydro-2H-pyridine
—— 2-(2,5-dimethyl-pyrrol-1-yl)-4-methyl-pyridine 95337-78-3 C12H14N2
2-(2,5-dimethyl-pyrrol-1-yl)-4-methyl-pyridine
—— (5-methyl-pyridin-2-yl)-acetic acid hydrochloride 848093-05-0 C8H9NO2*ClH
(5-methyl-pyridin-2-yl)-acetic acid hydrochloride
—— 3-tert-butylcyclohexanol 4534-70-7 C10H20O
3-tert-butylcyclohexanol
—— 4-(7-bromo-1-ethylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine 607370-99-0 C10H9BrN6O
4-(7-bromo-1-ethylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine
—— trans-4-isopropyl cyclohexanol 15890-36-5 C9H18O
trans-4-isopropyl cyclohexanol
—— dibenzyl 4,10-bis(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,7-dicarboxylate 187240-78-4 C36H52N4O8
dibenzyl 4,10-bis(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,7-dicarboxylate
—— (3,5-dinitrophenyl)morpholinylmethanone 133339-10-3 C11H11N3O6
(3,5-dinitrophenyl)morpholinylmethanone
—— 4-{trans-4-[(1E)-1-Propen-1-yl]cyclohexyl}benzonitrile 96184-40-6 C16H19N
4-{trans-4-[(1E)-1-Propen-1-yl]cyclohexyl}benzonitrile
—— [(1R,7R,8R,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]methanol 1139-17-9 C15H26O
[(1R,7R,8R,9S)-3,3,7-trimethyl-8-tricyclo[5.4.0.02,9]undecanyl]methanol
—— (<i>R</i>)-(2-hydroxy-propyl)-trimethyl-ammonium; chloride 2382-43-6 C6H16NO*Cl
(<i>R</i>)-(2-hydroxy-propyl)-trimethyl-ammonium; chloride
—— 109-06-8 C6H7N
—— 2-chloromethyl-8-hydroxy-4H-pyrido<1,2-a>pyrimidin-4-one 162469-86-5 C9H7ClN2O2
2-chloromethyl-8-hydroxy-4H-pyrido<1,2-a>pyrimidin-4-one
—— pyrimidine radical cation 289-95-2 C4H4N2
pyrimidine radical cation
—— 2-Isopropylthieno[3,2-d]pyrimidine-4-ol 443149-44-8 C9H10N2OS
2-Isopropylthieno[3,2-d]pyrimidine-4-ol
—— uracil-5-carboxylate decarboxylase 59299-01-3 —— ——
—— (3-Methylpyridin-2-yl)methanaminium 153936-26-6 C7H11N2+
(3-Methylpyridin-2-yl)methanaminium
—— (2,2-Dimethyl-5-oxo-1,3-dioxolan-4-yl)acetate 73991-95-4 C7H9O5-
(2,2-Dimethyl-5-oxo-1,3-dioxolan-4-yl)acetate
—— (2-Oxopyridin-1(2H)-yl)acetate 56546-36-2 C7H6NO3-
(2-Oxopyridin-1(2H)-yl)acetate
—— 2,5-Dimethylthiophene-3-carboxylate 26421-32-9 C7H7O2S-
2,5-Dimethylthiophene-3-carboxylate
—— Coronaridin 467-77-6 C21H26N2O2
Coronaridin
—— Bromadol 77239-98-6 C22H28BrNO
Bromadol
—— Gadolinium;2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid 72573-82-1 C16H28GdN4O8
Gadolinium;2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid
—— 4-(Carboxy{[(4-ethyl-2,3-dioxopiperazin-1-yl)(hydroxy)methylidene]amino}methyl)phenolate 62893-24-7 C15H16N3O6-
4-(Carboxy{[(4-ethyl-2,3-dioxopiperazin-1-yl)(hydroxy)methylidene]amino}methyl)phenolate
—— Imidazo[1,2-a]pyridine-2-carboxylate 64951-08-2 C8H5N2O2-
Imidazo[1,2-a]pyridine-2-carboxylate
—— Ethyl 3-nitrilioalaninate 75470-88-1 C5H9N2O2+
Ethyl 3-nitrilioalaninate
—— 6-[6-(3-Hydroxyundeca-1,5-dienyl)pyridin-2-yl]hexane-1,5-diol 119477-85-9 C22H35NO3
6-[6-(3-Hydroxyundeca-1,5-dienyl)pyridin-2-yl]hexane-1,5-diol
—— 3-Aminopyridine-2-carboxaldehyde thiosemicarbazone 143621-35-6 C7H9N5S
3-Aminopyridine-2-carboxaldehyde thiosemicarbazone