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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
—— 3,3,7,8-tetramethyl-11-(3-phenoxyphenyl)-2,3,4,5,10,11-hexahydro-1H-dibenzo[b,e][1,4]diazepin-1-one 5748-34-5 C29H30N2O2
3,3,7,8-tetramethyl-11-(3-phenoxyphenyl)-2,3,4,5,10,11-hexahydro-1H-dibenzo[b,e][1,4]diazepin-1-one
—— 6-(Chloromethyl)-2-(3-methylphenyl)pyrimidin-4-ol 680214-71-5 C12H11ClN2O
6-(Chloromethyl)-2-(3-methylphenyl)pyrimidin-4-ol
—— 2-methyl-3H-quinolin-4-one 5660-24-2 C10H9NO
2-methyl-3H-quinolin-4-one
—— 3-Nitro-4-{[3-(trifluoromethyl)phenyl]-sulfanyl}benzenecarbaldehyde 851975-11-6 C14H8F3NO3S
3-Nitro-4-{[3-(trifluoromethyl)phenyl]-sulfanyl}benzenecarbaldehyde
—— methyl 6-(1H-pyrrol-1-yl)nicotinate 852180-80-4 C11H10N2O2
methyl 6-(1H-pyrrol-1-yl)nicotinate
—— 6-(Methoxymethyl)-2-(3-methylphenyl)pyrimidin-4-ol 883032-71-1 C13H14N2O2
6-(Methoxymethyl)-2-(3-methylphenyl)pyrimidin-4-ol
—— Sodium 5-bromo-4-chloro-1H-indol-3-yl phosphate 102185-33-1 C8H4BrClNNa2O4P
Sodium 5-bromo-4-chloro-1H-indol-3-yl phosphate
—— (3S,4S)-1-(tert-butoxycarbonyl)-3-methylpiperidine-4-carboxylic acid 1207267-93-3 C12H21NO4
(3S,4S)-1-(tert-butoxycarbonyl)-3-methylpiperidine-4-carboxylic acid
—— 2-chloro-5-(1H-pyrazol-1-ylmethyl)pyridine 955966-95-7 C9H8ClN3
2-chloro-5-(1H-pyrazol-1-ylmethyl)pyridine
—— (Z)-2-cyano-3-morpholin-4-ylprop-2-enamide 25229-97-4 C8H11N3O2
(Z)-2-cyano-3-morpholin-4-ylprop-2-enamide
—— 4-t-Butyl-2-hydroxy-pyrimidin 17322-03-1 C8H12N2O
4-t-Butyl-2-hydroxy-pyrimidin
—— 1-[4-(2-Chloro-benzyl)-piperazin-1-yl]-3-methyl-butan-1-one 5932-27-4 C16H23ClN2O
1-[4-(2-Chloro-benzyl)-piperazin-1-yl]-3-methyl-butan-1-one
—— (3R)-3-hydroxy-3H-2-benzofuran-1-one 16859-59-9 C8H6O3
(3R)-3-hydroxy-3H-2-benzofuran-1-one
—— 3-Ethyl-s-triazolo<4,3-a>pyrazin 33590-18-0 C7H8N4
3-Ethyl-s-triazolo<4,3-a>pyrazin
—— Inosine 2',3',5'-tribenzoate 6741-88-4 C31H24N4O8
Inosine 2',3',5'-tribenzoate
—— N-α-trimethylhistidine 534-30-5 C9H16N3O2
N-α-trimethylhistidine
—— 1-allylindene 20258-77-9 C12H12
1-allylindene
—— (2R,4S)-2,4-pentanediol 3950-21-8 C5H12O2
(2R,4S)-2,4-pentanediol
—— 5,7-dimethyl-2-phenylquinoline 1075185-76-0 C17H15N
5,7-dimethyl-2-phenylquinoline
—— 2,3-dihydropyridin-4(1H)-one 24681-60-5 C5H7NO
2,3-dihydropyridin-4(1H)-one
—— methyl 5-methoxypyrazolo[1,5-a]pyridine-3-carboxylate 99446-31-8 C10H10N2O3
methyl 5-methoxypyrazolo[1,5-a]pyridine-3-carboxylate
—— 3,5-dimethyl pyridine cation 591-22-0 C7H9N
3,5-dimethyl pyridine cation
—— 4-iodo-4'-methoxybiphenyl 126971-87-7 C13H11IO
4-iodo-4'-methoxybiphenyl
—— 4-Bromo-8-iodoquinoline 608143-12-0 C9H5BrIN
4-Bromo-8-iodoquinoline
—— 1-{6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-3-pyridinyl}-2-pyrrolidinone 720691-69-0 C23H27N3O2
1-{6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-3-pyridinyl}-2-pyrrolidinone
—— N8Jtw437BS 886025-85-0 C13H17N3O3
N8Jtw437BS
—— 2-(3-chlorophenyl)piperidine 383128-12-9 C11H14ClN
2-(3-chlorophenyl)piperidine
—— (2,4-dinitro-phenylsulfanyl)-acetic acid ethyl ester 85196-28-7 C10H10N2O6S
(2,4-dinitro-phenylsulfanyl)-acetic acid ethyl ester
—— [N<sub>4444</sub>][2-OP] 880762-06-1 C5H4NO*C16H36N
[N<sub>4444</sub>][2-OP]
—— 1-((4-methoxybenzyl)amino)propan-2-ol 856978-80-8 C11H17NO2
1-((4-methoxybenzyl)amino)propan-2-ol
—— (+/-)-trans-3-hydroxycyclohexanecarboxylic acid 21531-44-2 C7H12O3
(+/-)-trans-3-hydroxycyclohexanecarboxylic acid
—— 5-bromo-3,3-dimethylisobenzofuran-1(3H)-one 1029696-37-4 C10H9BrO2
5-bromo-3,3-dimethylisobenzofuran-1(3H)-one
—— 5-(bromomethyl)-2-chloropyrimidine 153281-13-1 C5H4BrClN2
5-(bromomethyl)-2-chloropyrimidine
—— 2-aza-bicyclo[3.1.0]hexane-2-carboxylic acid benzyl ester 841302-36-1 C13H15NO2
2-aza-bicyclo[3.1.0]hexane-2-carboxylic acid benzyl ester
—— 4-bromo-6-chloro-2,3-dihydro-1H-inden-1-one 1260017-94-4 C9H6BrClO
4-bromo-6-chloro-2,3-dihydro-1H-inden-1-one
—— 3-Hydroxyanagrelide 733043-41-9 C10H7Cl2N3O2
3-Hydroxyanagrelide
—— Neoprotoveratrine 124-97-0 C41H63NO15
Neoprotoveratrine
—— 5-methyl-2,3-dihydro-1,4-benzodioxin 33632-34-7 C9H10O2
5-methyl-2,3-dihydro-1,4-benzodioxin
—— 4-fluoro-pyrrole-2-carboxylic acid 475561-90-1 C5H4FNO2
4-fluoro-pyrrole-2-carboxylic acid
—— 6-Hydroxy-1,2,3,4-tetrahydro-3-isoquinolinecarboxylic acid hydrate 134388-87-7 C10H13NO4
6-Hydroxy-1,2,3,4-tetrahydro-3-isoquinolinecarboxylic acid hydrate
—— -(3,3-dimethyl-1-buten-1-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 154820-99-2 C12H23BO2
-(3,3-dimethyl-1-buten-1-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
—— 4-(dimethylamino)-1,2,2,6,6-pentamethyl-piperidine 52185-74-7 C12H26N2
4-(dimethylamino)-1,2,2,6,6-pentamethyl-piperidine
—— 3-nitropyrazolo[1,5-a]pyridine 19363-97-4 C7H5N3O2
3-nitropyrazolo[1,5-a]pyridine
—— bis(2-methoxyphenyl)phosphine oxide 71360-04-8 C14H15O3P
bis(2-methoxyphenyl)phosphine oxide
—— 3-({[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}sulfanyl)-5,5-dimethyl-4,5-dihydro-1,2-oxazole 656825-92-2 C12H14F5N3O2S
3-({[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}sulfanyl)-5,5-dimethyl-4,5-dihydro-1,2-oxazole
—— (5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl)-quinolin-4-ylmethanol;dihydrochloride 24302-67-8 C19H24Cl2N2O
(5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl)-quinolin-4-ylmethanol;dihydrochloride
—— (2S,3S,4S,5R)-3,4,5-Trihydroxy-6-(quinolin-8-yloxy)tetrahydro-2H-pyran-2-carboxylic acid 14683-61-5 C15H15NO7
(2S,3S,4S,5R)-3,4,5-Trihydroxy-6-(quinolin-8-yloxy)tetrahydro-2H-pyran-2-carboxylic acid
—— di-tert-butyl (2-oxopropane-1,3-diyl)dicarbamate 129758-92-5 C13H24N2O5
di-tert-butyl (2-oxopropane-1,3-diyl)dicarbamate
—— 4-tert-butyl-2,6-diiodoaniline 173282-39-8 C10H13I2N
4-tert-butyl-2,6-diiodoaniline
—— 4-(2-ethylhexyl)-4H-thieno[3,2-b]pyrrole-5,6-dione 1147124-46-6 C14H19NO2S
4-(2-ethylhexyl)-4H-thieno[3,2-b]pyrrole-5,6-dione