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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
—— (3a<i>S</i>)-1<i>c</i>-(4-β-D-Glucopyranosyloxy-3-methoxy-phenyl)-4<i>t</i>-(4-hydroxy-3-methoxy-phenyl)-(3a<i>r</i>,6a<i>c</i>)-tetrahydro-furo[3,4-<i>c</i>]furan 24404-49-7 C26H32O11
(3a<i>S</i>)-1<i>c</i>-(4-β-D-Glucopyranosyloxy-3-methoxy-phenyl)-4<i>t</i>-(4-hydroxy-3-methoxy-phenyl)-(3a<i>r</i>,6a<i>c</i>)-tetrahydro-furo[3,4-<i>c</i>]furan
—— benzyl 2-acetamido-2-deoxy-3,6-di-O-benzyl-β-D-glucopyranoside 62867-63-4 C29H33NO6
benzyl 2-acetamido-2-deoxy-3,6-di-O-benzyl-β-D-glucopyranoside
—— 7β-amino-7α-methoxy-3-[[(1-methyl-1H-triazol-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-triazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid diphenylmethyl ester
—— 1α,3β-bis<(tert-butyldimethylsilyl)oxy>-23,24-bisnorchol-5,7-dien-22-ol 126771-88-8 C34H62O3Si2
1α,3β-bis<(tert-butyldimethylsilyl)oxy>-23,24-bisnorchol-5,7-dien-22-ol
—— 1α,3β-bis[(tert-butyldimethylsilyl)oxy]-5α,8α-(3,5-dioxo-4-phenyl-1,2,4-triazolidine-1,2-diyl)-23,24-bisnorchol-6-en-22-ol 174201-34-4 C42H67N3O5Si2
1α,3β-bis[(tert-butyldimethylsilyl)oxy]-5α,8α-(3,5-dioxo-4-phenyl-1,2,4-triazolidine-1,2-diyl)-23,24-bisnorchol-6-en-22-ol
—— 5-fluoro-6-methylthioindole 259860-09-8 C9H8FNS
5-fluoro-6-methylthioindole
—— 2,5-bis(2-(2-methoxyethoxy)ethoxy)terephthalaldehyde 1628897-24-4 C18H26O8
2,5-bis(2-(2-methoxyethoxy)ethoxy)terephthalaldehyde
—— 7-(2-Bromo-acetylamino)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid 58197-02-7 C10H11BrN2O4S
7-(2-Bromo-acetylamino)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
—— 2,8-dichloro-10H-phenothiazine 1730-45-6 C12H7Cl2NS
2,8-dichloro-10H-phenothiazine
—— 4-chloro-2-methyl-2H-pyrazolo[3,4-d]pyrimidine 959430-67-2 C6H5ClN4
4-chloro-2-methyl-2H-pyrazolo[3,4-d]pyrimidine
—— 1-(tert-butyl) 2-methyl (2S,4S)-4-hydroxypiperidine-1,2-dicarboxylate 254882-14-9 C12H21NO5
1-(tert-butyl) 2-methyl (2S,4S)-4-hydroxypiperidine-1,2-dicarboxylate
—— 1-methoxy-3,5-diamino-benzene 100-96-9 C7H10N2O
1-methoxy-3,5-diamino-benzene
—— tert-butyl 2-(4-hydroxypiperidin-1-yl)acetate 166955-02-8 C11H21NO3
tert-butyl 2-(4-hydroxypiperidin-1-yl)acetate
—— 2-hydroxy-2-methyl-2-(4'-methylphenyl)acetonitrile 69813-74-7 C10H11NO
2-hydroxy-2-methyl-2-(4'-methylphenyl)acetonitrile
—— methyl pyrrolo<3,2-e>indole-2-carboxylate 107474-65-7 C12H10N2O2
methyl pyrrolo<3,2-e>indole-2-carboxylate
—— 4-Hydroxy-2,5-dihydrothiophene-3-carbonitrile 16563-14-7 C5H5NOS
4-Hydroxy-2,5-dihydrothiophene-3-carbonitrile
—— 1,3,5-tris(methoxymethyl)benzene 84941-01-5 C12H18O3
1,3,5-tris(methoxymethyl)benzene
—— bis[4-(acryloyloxyethyl)thiophenyl]sulfide 133811-67-3 C22H22O4S3
bis[4-(acryloyloxyethyl)thiophenyl]sulfide
—— ethyl 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)-5-(4-nitrophenyl)thiophene-3-carboxylate 308832-01-1 C28H31F2N3O7S
ethyl 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)-5-(4-nitrophenyl)thiophene-3-carboxylate
—— 5-nitroisoindolin-1-one 110568-64-4 C8H6N2O3
5-nitroisoindolin-1-one
—— 4-chromanol 120523-16-2 C9H10O2
4-chromanol
—— 6-methoxy-2-(diphenylphosphino)pyridine 132682-80-5 C18H16NOP
6-methoxy-2-(diphenylphosphino)pyridine
—— methyl 6-chloro-3-nitropyrazinoate 89690-75-5 C6H4ClN3O4
methyl 6-chloro-3-nitropyrazinoate
—— tert-butyl (2S,4R)-2-(hydroxymethyl)-4-methylpyrrolidine-1-carboxylate 220047-75-6 C11H21NO3
tert-butyl (2S,4R)-2-(hydroxymethyl)-4-methylpyrrolidine-1-carboxylate
—— 5’-O-DMT-N2-isobutyrylguanosine 81246-83-5 C35H37N5O8
5’-O-DMT-N2-isobutyrylguanosine
—— (3aR,4R,5R,6aS)-benzoic acid 2-oxo-4-[(1E)-3-oxo-oct-1-enyl]-hexahydro-cyclopenta[b]furan-5-yl ester 40834-86-4 C22H26O5
(3aR,4R,5R,6aS)-benzoic acid 2-oxo-4-[(1E)-3-oxo-oct-1-enyl]-hexahydro-cyclopenta[b]furan-5-yl ester
—— n-Methyl-4-(p-formylstyryl)pyridinium methylsulfate 74401-04-0 C16H17NO5S
n-Methyl-4-(p-formylstyryl)pyridinium methylsulfate
—— 4-(4-pyridylmethyl)-1-piperazinecarboxylic acid, ethyl ester 143210-48-4 C13H19N3O2
4-(4-pyridylmethyl)-1-piperazinecarboxylic acid, ethyl ester
—— 2-(pyrimidin-4-yl)nicotinic acid 1429555-05-4 C10H7N3O2
2-(pyrimidin-4-yl)nicotinic acid
—— (2R)-1,4-dioxan-2-yl-N-methylmethanaminium chloride 917882-58-7 C6H13NO2*ClH
(2R)-1,4-dioxan-2-yl-N-methylmethanaminium chloride
—— 6-(7-methoxyquinolin-4-yloxy)-1-naphthoic acid 847803-42-3 C21H15NO4
6-(7-methoxyquinolin-4-yloxy)-1-naphthoic acid
—— Nopinon 24903-95-5 C9H14O
Nopinon
—— 4-[4-(trifluoromethyl)-phenoxy]piperidine 28033-37-6 C12H14F3NO
4-[4-(trifluoromethyl)-phenoxy]piperidine
—— biphenyl-2-yl-carbamic acid 1-[2-(benzylmethylamino)ethyl]piperidin-4-yl ester 864686-28-2 C28H33N3O2
biphenyl-2-yl-carbamic acid 1-[2-(benzylmethylamino)ethyl]piperidin-4-yl ester
—— 4,4'-biphenyldiol bis[di(2,6-dimethylphenyl)phosphate] 147263-99-8 C44H44O8P2
4,4'-biphenyldiol bis[di(2,6-dimethylphenyl)phosphate]
—— 1-docosyl-piperazine 1018908-25-2 C26H54N2
1-docosyl-piperazine
—— benzyl N-(2,2-dimethoxyethyl)-N-methyl-carbamate 1355573-66-8 C13H19NO4
benzyl N-(2,2-dimethoxyethyl)-N-methyl-carbamate
—— 2-(4-(tert-butyl)phenyl)quinoline 917114-13-7 C19H19N
2-(4-(tert-butyl)phenyl)quinoline
—— 2-cyclopropyl-6-oxo-1,6-dihydropyrimidine-4-carboxylic acid 858956-25-9 C8H8N2O3
2-cyclopropyl-6-oxo-1,6-dihydropyrimidine-4-carboxylic acid
—— [(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] (4aS,6aS,6bR,10S,12aR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylate 14162-53-9 C36H58O8
[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] (4aS,6aS,6bR,10S,12aR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylate
—— oleanolic acid 28-O-β-D-glucopyranosyl ester 14162-53-9 C36H58O8
oleanolic acid 28-O-β-D-glucopyranosyl ester
—— 1-((3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)pyrrolidine 1509932-05-1 C16H24BNO4S
1-((3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)pyrrolidine
—— 2,3,5-trimethylcyclohexanol 116-02-9 C9H18O
2,3,5-trimethylcyclohexanol
—— 1-benzyl-4-amino-piperidine dihydrochloride 1205-72-7 C12H18N2*2ClH
1-benzyl-4-amino-piperidine dihydrochloride
—— 5-hydroxy-2-(tetrahydro-2H-pyran-2-yl)pyridazin-3(2H)-one 1008517-74-5 C9H12N2O3
5-hydroxy-2-(tetrahydro-2H-pyran-2-yl)pyridazin-3(2H)-one
—— 3-Bromo-6-nonanylthieno[3,2-b]thiophene 763115-01-1 C15H21BrS2
3-Bromo-6-nonanylthieno[3,2-b]thiophene
—— 2-(3-bromophenyl)dibenzofuran 1084334-27-9 C18H11BrO
2-(3-bromophenyl)dibenzofuran
—— 6-methyl-2-(phenylmethoxy)benzoic acid 118537-95-4 C15H14O3
6-methyl-2-(phenylmethoxy)benzoic acid
—— per-6-thio-β-cyclodextrin 160661-60-9 C42H70O28S7
per-6-thio-β-cyclodextrin
—— 5-METHYL-2-PYRIDYLZINC BROMIDE 257876-05-4 C6H6BrNZn
5-METHYL-2-PYRIDYLZINC BROMIDE