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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
—— (2S)-2-amino-N-[(1S)-2-[4-(hydroxymethyl)anilino]-1-methyl-2-oxoethyl]-3-methylbutanamide 1343476-44-7 C15H23N3O3
(2S)-2-amino-N-[(1S)-2-[4-(hydroxymethyl)anilino]-1-methyl-2-oxoethyl]-3-methylbutanamide
—— 6-bromo-3-iodo-2-methoxypyridine 1310949-37-1 C6H5BrINO
6-bromo-3-iodo-2-methoxypyridine
—— 4-cyanocyclohexane-1-carboxylic acid 15177-68-1 C8H11NO2
4-cyanocyclohexane-1-carboxylic acid
—— 3-(chloromethyl)-2-cyclopropyl-4-(4-fluorophenyl)quinoline 1234331-56-6 C19H15ClFN
3-(chloromethyl)-2-cyclopropyl-4-(4-fluorophenyl)quinoline
—— 1,4-Piperazinedicarbodithioic acid, dipotassium salt 40839-73-4 C6H8N2S4*2K
1,4-Piperazinedicarbodithioic acid, dipotassium salt
—— cis-1-(tert-Butoxycarbonyl)-4-hydroxypiperidine-3-carboxylic acid 194795-71-6 C11H19NO5
cis-1-(tert-Butoxycarbonyl)-4-hydroxypiperidine-3-carboxylic acid
—— (S)-tert-Butyl 6-(aminomethyl)-2,2-dimethylmorpholine-4-carboxylate oxalate 1951425-14-1 C14H26N2O7
(S)-tert-Butyl 6-(aminomethyl)-2,2-dimethylmorpholine-4-carboxylate oxalate
—— tert-Butyl-N-(3-pyridyl)glycinate 710939-70-1 C11H16N2O2
tert-Butyl-N-(3-pyridyl)glycinate
—— (1R,3R,4R)-3-hydroxy-4-mercapto-cyclohexylcarbamic acid tert-butyl ester 1350636-75-7 C11H21NO3S
(1R,3R,4R)-3-hydroxy-4-mercapto-cyclohexylcarbamic acid tert-butyl ester
—— tert-butyl N-[(1R,3R,4R)-4-(benzoylsulfanyl)-3-hydroxycyclohexyl]carbamate 1350636-89-3 C18H25NO4S
tert-butyl N-[(1R,3R,4R)-4-(benzoylsulfanyl)-3-hydroxycyclohexyl]carbamate
—— 3,3,20,20-bis(ethylene-dioxy)-5α-17α-dihydroxy-11β-[4-(N,N-dimethylamino)-phenyl-]-19-norpregna-9(11)-ene 126690-41-3 C32H45NO6
3,3,20,20-bis(ethylene-dioxy)-5α-17α-dihydroxy-11β-[4-(N,N-dimethylamino)-phenyl-]-19-norpregna-9(11)-ene
—— {(1R,2R,4R)-4-[(2,2,2-trifluoro-acetyl)-amino]-2-hydroxy-cyclohexyl} benzene-carbothioate 1350636-92-8 C15H16F3NO3S
{(1R,2R,4R)-4-[(2,2,2-trifluoro-acetyl)-amino]-2-hydroxy-cyclohexyl} benzene-carbothioate
—— 1,3-Dithietane-2-carboxylic acid, 4-[1-(aminocarbonyl)-2-(1,1-dimethylethoxy)-2-oxoethylidene]- 955010-42-1 C10H13NO5S2
1,3-Dithietane-2-carboxylic acid, 4-[1-(aminocarbonyl)-2-(1,1-dimethylethoxy)-2-oxoethylidene]-
—— oxidized DTT 14193-38-5 C4H8O2S2
oxidized DTT
—— N-acetyl-2,4,7,8,9-penta-O-acetyl-D-neuraminic acid 4887-11-0 C21H29NO14
N-acetyl-2,4,7,8,9-penta-O-acetyl-D-neuraminic acid
—— 2,3,4-tri-O-acetyl-D-xylopyranosyl trichloroacetimidate 197144-02-8 C13H16Cl3NO8
2,3,4-tri-O-acetyl-D-xylopyranosyl trichloroacetimidate
—— 2,2'-bithiophene-3,3'-dicarboxylic acid 19690-71-2 C10H6O4S2
2,2'-bithiophene-3,3'-dicarboxylic acid
—— 4985-25-5 C4H10N2*C19H19N2O2*H
—— (E)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-6-yl)thio)benzamide 885126-35-2 C27H26N4O2S
(E)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-6-yl)thio)benzamide
—— (E)-6-nitro-3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole 886230-75-7 C19H18N4O3
(E)-6-nitro-3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole
—— 9-(biphenyl-3-yl)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-9H-carbazole 1533406-38-0 C30H28BNO2
9-(biphenyl-3-yl)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-9H-carbazole
—— MOE 5-Me-C Amidite 163759-94-2 C50H60N5O10P
MOE 5-Me-C Amidite
—— pyrazine-2,5-dicarboxylic acid dihydrate 205692-63-3 C6H4N2O4*2H2O
pyrazine-2,5-dicarboxylic acid dihydrate
—— 3,3-difluorocyclohexane-1-carboxylic acid 849669-20-1 C7H10F2O2
3,3-difluorocyclohexane-1-carboxylic acid
—— 1-ethylpyridinium bis(trifluoromethylsulfonyl)imide 712354-97-7 C2F6NO4S2*C7H10N
1-ethylpyridinium bis(trifluoromethylsulfonyl)imide
—— 8-fluoroquinolin-3-amine 936324-21-9 C9H7FN2
8-fluoroquinolin-3-amine
—— 5-chlorothiazolo[5,4-d]pyrimidin-2-amine 1006879-06-6 C5H3ClN4S
5-chlorothiazolo[5,4-d]pyrimidin-2-amine
—— (3R,4R)-1-(tert-butoxycarbonyl)-3-methylpiperidine-4-carboxylic acid 1207267-93-3 C12H21NO4
(3R,4R)-1-(tert-butoxycarbonyl)-3-methylpiperidine-4-carboxylic acid
—— methyl 4-(2-methoxyphenyl)-2,4-dioxobutanoate 848052-89-1 C12H12O5
methyl 4-(2-methoxyphenyl)-2,4-dioxobutanoate
—— trans-(4-tert-butoxycarbonylamino-cyclohexyl)-acetic acid ethyl ester 946598-34-1 C15H27NO4
trans-(4-tert-butoxycarbonylamino-cyclohexyl)-acetic acid ethyl ester
—— (3-aminobicyclo[1.1.1]pentan-1-yl)methanol hydrochloride 1638767-26-6 C6H11NO*ClH
(3-aminobicyclo[1.1.1]pentan-1-yl)methanol hydrochloride
—— 2-(5-bromopyrimidin-2-yl)propan-2-ol 1193244-89-1 C7H9BrN2O
2-(5-bromopyrimidin-2-yl)propan-2-ol
—— (E)-4-bromo-N-hydroxybenzimidoyl chloride 29203-58-5 C7H5BrClNO
(E)-4-bromo-N-hydroxybenzimidoyl chloride
—— 2-bromo-1,3-dichloro-5-iodobenzene 1000574-29-7 C6H2BrCl2I
2-bromo-1,3-dichloro-5-iodobenzene
—— (R)-3-piperidinecarboxylic acid ethyl ester (+)-tartrate 167392-57-6 C4H6O6*C8H15NO2
(R)-3-piperidinecarboxylic acid ethyl ester (+)-tartrate
—— 5-[5-oxo-8-[6-(4-piperidyloxy)-3-pyridyl]-7-thioxo-6,8-diazaspiro[3.4]octan-6-yl]-3-(trifluoromethyl)pyridine-2-carbonitrile 2110426-27-0 C23H21F3N6O2S
5-[5-oxo-8-[6-(4-piperidyloxy)-3-pyridyl]-7-thioxo-6,8-diazaspiro[3.4]octan-6-yl]-3-(trifluoromethyl)pyridine-2-carbonitrile
—— 5-chloro-3-iodo-1H-pyrazolo[3,4-c]pyridine 1260666-29-2 C6H3ClIN3
5-chloro-3-iodo-1H-pyrazolo[3,4-c]pyridine
—— (4-chloro-2-(methoxycarbonyl)phenyl)boronic acid 1612256-37-7 C8H8BClO4
(4-chloro-2-(methoxycarbonyl)phenyl)boronic acid
—— tert-butyl 1H-pyrrole-3-carboxylate 741606-06-4 C9H13NO2
tert-butyl 1H-pyrrole-3-carboxylate
—— 6-chloro-3-isopropylpyrimidine-2,4(1H,3H)-dione 887581-47-7 C7H9ClN2O2
6-chloro-3-isopropylpyrimidine-2,4(1H,3H)-dione
—— (E)-N'-(2-cyano-4-nitrophenyl)-N,N'-dimethylformimidamide 39263-34-8 C10H10N4O2
(E)-N'-(2-cyano-4-nitrophenyl)-N,N'-dimethylformimidamide
—— 2-(4-bromophenyl)-2-oxoacetaldehyde hydrate 80352-42-7 C8H5BrO2*H2O
2-(4-bromophenyl)-2-oxoacetaldehyde hydrate
—— 4-[1-(1,3,4-triazolyl)methyl]-benzonitrile 112809-25-3 C10H8N4
4-[1-(1,3,4-triazolyl)methyl]-benzonitrile
—— (1R,5S,6s)-tert-butyl 6-amino-3-azabicyclo[3.1.0]hexane-3-carboxylate 273206-92-1 C10H18N2O2
(1R,5S,6s)-tert-butyl 6-amino-3-azabicyclo[3.1.0]hexane-3-carboxylate
—— (2S,5R)-ethyl 5-((benzyloxy)amino)piperidine-2-carboxylate 1416134-47-8 C15H22N2O3
(2S,5R)-ethyl 5-((benzyloxy)amino)piperidine-2-carboxylate
—— 4′,5′-bis(1,3,2-dithioarsolan-2-yl) fluorescein 212118-77-9 C24H18As2O5S4
4′,5′-bis(1,3,2-dithioarsolan-2-yl) fluorescein
—— 7-amino-3-(1-methyl-1H-tetrazole-5-ylthiomethyl)-3-cephem-4-carboxylic acid 24209-38-9 C10H12N6O3S2
7-amino-3-(1-methyl-1H-tetrazole-5-ylthiomethyl)-3-cephem-4-carboxylic acid
—— 5-(piperidin-4-yl)-1,3,4-thiadiazol-2-amine 881040-24-0 C7H12N4S
5-(piperidin-4-yl)-1,3,4-thiadiazol-2-amine
—— methyl 3-amino-1-methylpyrazole-4-carboxylate 64182-19-0 C6H9N3O2
methyl 3-amino-1-methylpyrazole-4-carboxylate
—— [1,2,4]triazolo[1,5-a]pyridine-7-carbaldehyde 1268521-09-0 C7H5N3O
[1,2,4]triazolo[1,5-a]pyridine-7-carbaldehyde