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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
—— 7-ethoxycarbonylmethyl-3,4-dihydro-2H-[1,8]naphthyridine-1-carboxylic acid tert-butyl ester 243641-38-5 C17H24N2O4
7-ethoxycarbonylmethyl-3,4-dihydro-2H-[1,8]naphthyridine-1-carboxylic acid tert-butyl ester
—— ethyl 2-(3,4,5-trimethoxybenzamido)thiazole-4-carboxylate 397277-84-8 C16H18N2O6S
ethyl 2-(3,4,5-trimethoxybenzamido)thiazole-4-carboxylate
—— crotonic acid sec-butyl ester 10371-45-6 C8H14O2
crotonic acid sec-butyl ester
—— tert-butyl 1-aminocyclopropane-1-carboxylate 159871-51-9 C8H15NO2
tert-butyl 1-aminocyclopropane-1-carboxylate
—— Eltrombopag olamine 496775-62-3 C29H36N6O6
Eltrombopag olamine
—— 2,6-diphenylbenzaldehyde 169618-84-2 C19H14O
2,6-diphenylbenzaldehyde
—— methyl (3-bromo-5-formyl-4-hydroxyphenyl)acetate 277313-22-1 C10H9BrO4
methyl (3-bromo-5-formyl-4-hydroxyphenyl)acetate
—— (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide 1337918-83-8 C36H46N8O3
(R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide
—— 4-cyano-4-(3-methoxyphenyl)-3,4,5,6-tetrahydro-2H-pyran 179420-73-6 C13H15NO2
4-cyano-4-(3-methoxyphenyl)-3,4,5,6-tetrahydro-2H-pyran
—— bis(benzo[d][1,3]dioxol-5-yl)(piperidin-4-yl)methanol 1446818-43-4 C20H21NO5
bis(benzo[d][1,3]dioxol-5-yl)(piperidin-4-yl)methanol
—— 5-bromo-1H-pyrazolo[3,4-b]pyrazine 1196152-90-5 C5H3BrN4
5-bromo-1H-pyrazolo[3,4-b]pyrazine
—— 4,4'-di-tert-butyl-6-phenyl-2,2'-bipyridine 693263-19-3 C24H28N2
4,4'-di-tert-butyl-6-phenyl-2,2'-bipyridine
—— 2-Amino-6-(hydroxymethyl)pyrimidin-4(1H)-one 253340-48-6 C5H7N3O2
2-Amino-6-(hydroxymethyl)pyrimidin-4(1H)-one
—— Pyrrolidinyl diaminopyrimidine oxide 55921-65-8 C8H13N5O
Pyrrolidinyl diaminopyrimidine oxide
—— 2-isopropyl-1-methyl-pyrrolidine 77972-88-4 C8H17N
2-isopropyl-1-methyl-pyrrolidine
—— 2-Aminomethyl-7-chloro-2,3-dihydro-5-(2-fluorophenyl)-1H-1,4-benzodiazepine Dimaleate 59469-29-3 C24H23ClFN3O8
2-Aminomethyl-7-chloro-2,3-dihydro-5-(2-fluorophenyl)-1H-1,4-benzodiazepine Dimaleate
—— 6-bromo-3,3-dimethyl-2,3-dihydro-pyrrolo[3,2-b]pyridine-1-carboxylic acid tert-butyl ester 1403901-49-4 C14H19BrN2O2
6-bromo-3,3-dimethyl-2,3-dihydro-pyrrolo[3,2-b]pyridine-1-carboxylic acid tert-butyl ester
—— 2,7-dibromobenzo[1,2-b:6,5-b']dithiophene-4,5-dione 1258459-49-2 C10H2Br2O2S2
2,7-dibromobenzo[1,2-b:6,5-b']dithiophene-4,5-dione
—— 4,6-diphenylpyrimidine 3977-48-8 C16H12N2
4,6-diphenylpyrimidine
—— tert-butyl 7-(bromomethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate 1158756-43-4 C15H20BrNO2
tert-butyl 7-(bromomethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate
—— (S)-3-((tert-butoxycarbonyl)(isopropyl)amino)-2-(4-chlorophenyl)propionic acid 1001179-33-4 C17H24ClNO4
(S)-3-((tert-butoxycarbonyl)(isopropyl)amino)-2-(4-chlorophenyl)propionic acid
—— 4,4,9,9-tetrahexadecyl-4,9-dihydro-s-indaceno[1,2-b:5,6-b']dithiophene 1209012-34-9 C80H138S2
4,4,9,9-tetrahexadecyl-4,9-dihydro-s-indaceno[1,2-b:5,6-b']dithiophene
—— 3-methyl-trans(3-fluorocyclobutanecarboxylic acid) 1455037-43-0 C6H9FO2
3-methyl-trans(3-fluorocyclobutanecarboxylic acid)
—— ethyl 3-nitro-4-piperidin-1-ylbenzoate 71254-72-3 C14H18N2O4
ethyl 3-nitro-4-piperidin-1-ylbenzoate
—— dimethyl 4,5-dimethylphthalate 17649-59-1 C12H14O4
dimethyl 4,5-dimethylphthalate
—— methyl 4-<N-<(tert-butyloxy)carbonyl>piperidin-4-yl>butanoate 142355-82-6 C15H27NO4
methyl 4-<N-<(tert-butyloxy)carbonyl>piperidin-4-yl>butanoate
—— (4-nitrophenyl)methyl (NZ)-N-[1-[(3S)-3-sulfanylpyrrolidin-1-yl]ethylidene]carbamate 90505-36-5 C14H17N3O4S
(4-nitrophenyl)methyl (NZ)-N-[1-[(3S)-3-sulfanylpyrrolidin-1-yl]ethylidene]carbamate
—— 8-[bis(chlorophenyl)methyl]-8-azabicyklo[3.2.1]octan-3-one 524019-24-7 C20H19Cl2NO
8-[bis(chlorophenyl)methyl]-8-azabicyklo[3.2.1]octan-3-one
—— 3-[4-(aminomethyl)-1-oxo-1,3-dihydro-isoindol-2-yl]piperidine-2,6-dione hydrochloride 444289-05-8 C14H15N3O3*ClH
3-[4-(aminomethyl)-1-oxo-1,3-dihydro-isoindol-2-yl]piperidine-2,6-dione hydrochloride
—— (S)-5-(morpholine-4-carbonyl)pyrrolidin-2-one 85187-29-7 C9H14N2O3
(S)-5-(morpholine-4-carbonyl)pyrrolidin-2-one
—— 5-{-4-[2-(N-methyl-N-(2-pyridyl)-amino)-ethoxy]-benzylidene}-2,4-thiazolidinedione 122320-74-5 C18H17N3O3S
5-{-4-[2-(N-methyl-N-(2-pyridyl)-amino)-ethoxy]-benzylidene}-2,4-thiazolidinedione
—— ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate 944559-46-0 C12H15NO3S
ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate
—— ethyl 2-(aminooxy)-acetate 5740-47-6 C4H9NO3
ethyl 2-(aminooxy)-acetate
—— 2,6-bis(diphenylphosphinomethyl)pyridine 73892-45-2 C31H27NP2
2,6-bis(diphenylphosphinomethyl)pyridine
—— 2-Aminopyridine <i>N</i>-Oxide 14150-95-9 C5H6N2O
2-Aminopyridine <i>N</i>-Oxide
—— (R)-3-ethylcyclopentanone 10264-55-8 C7H12O
(R)-3-ethylcyclopentanone
—— (S)-3-ethylcyclopentanone 10264-55-8 C7H12O
(S)-3-ethylcyclopentanone
—— 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxylic acid 1050477-45-6 C21H21N3O4
4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxylic acid
—— 2-cyanoethyl 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxylate 1050477-44-5 C24H24N4O4
2-cyanoethyl 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxylate
—— 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide 1050477-27-4 C21H22N4O3
4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
—— 1,1'-(oxydiethane-2,1-diyl)bis(1H-imidazole) 134443-67-7 C10H14N4O
1,1'-(oxydiethane-2,1-diyl)bis(1H-imidazole)
—— 3,4-di-O-isopropylidene-D-mannitol 3969-84-4 C9H18O6
3,4-di-O-isopropylidene-D-mannitol
—— 2-azidoethyl α-D-mannopyranoside 155196-97-7 C8H15N3O6
2-azidoethyl α-D-mannopyranoside
—— adenylyl 3'-5' cytidine 4833-63-0 C19H25N8O11P
adenylyl 3'-5' cytidine
—— (1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21Z,24S)-6'-Cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(4S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 165108-07-6 C43H63NO11
(1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21Z,24S)-6'-Cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(4S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— 2'-O-methoxyethyl- N<sup>6</sup>-benzoyl -adenosine 333335-93-6 C20H23N5O6
2'-O-methoxyethyl- N<sup>6</sup>-benzoyl -adenosine
—— trans-decahydroquinoline 767-92-0 C9H17N
trans-decahydroquinoline
—— tert-butyl N-[(2S)-1-[(2S)-2-[[(1R)-5-amino-1-[(1S,2S,6R,8S)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]pentyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-trimethylsilylpropan-2-yl]carbamate 171596-59-1 C31H57BN4O6Si
tert-butyl N-[(2S)-1-[(2S)-2-[[(1R)-5-amino-1-[(1S,2S,6R,8S)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]pentyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-trimethylsilylpropan-2-yl]carbamate
—— 5-(tert-butyldiphenylsilyl)-2,3-O-isopropylidene-D-ribono-1,4-lactone 130222-84-3 C24H30O5Si
5-(tert-butyldiphenylsilyl)-2,3-O-isopropylidene-D-ribono-1,4-lactone
—— ethyl 2-(chloromethyl)-4-phenylquinoline-3-carboxylate 126334-84-7 C19H16ClNO2
ethyl 2-(chloromethyl)-4-phenylquinoline-3-carboxylate