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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
—— 6-chloro-4-methyl-2H-chromen-2-one 24145-78-6 C10H7ClO2
6-chloro-4-methyl-2H-chromen-2-one
—— methyl 1-isopropyl-1H-indole-6-carboxylate 202745-76-4 C13H15NO2
methyl 1-isopropyl-1H-indole-6-carboxylate
—— CIS,CIS-1,3,5-CYCLOHEXANETRIOL DIHYDRATE 50409-12-6 C6H12O3
CIS,CIS-1,3,5-CYCLOHEXANETRIOL DIHYDRATE
—— trans-2,10-epoxypinane 6931-54-0 C10H16O
trans-2,10-epoxypinane
—— methyl (6aR,9R,10aR)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxylate 30341-92-5 C16H18N2O2
methyl (6aR,9R,10aR)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxylate
—— ethyl 2-amino-4-(3-chlorophenyl)thiophene-3-carboxylate 473438-03-8 C13H12ClNO2S
ethyl 2-amino-4-(3-chlorophenyl)thiophene-3-carboxylate
—— trans-4-Methylcyclohexyl amine 2523-55-9 C7H15N
trans-4-Methylcyclohexyl amine
—— 4-methoxyphenyl 4,6-O-benzylidene-β-D-galactopyranoside 176299-96-0 C20H22O7
4-methoxyphenyl 4,6-O-benzylidene-β-D-galactopyranoside
—— (6-chloro-4-(ethylamino)pyridin-3-yl)methanol 959162-99-3 C8H11ClN2O
(6-chloro-4-(ethylamino)pyridin-3-yl)methanol
—— N<sup>4</sup>-acetyl-2',3'-dideoxycytidine 119818-52-9 C11H15N3O4
N<sup>4</sup>-acetyl-2',3'-dideoxycytidine
—— 3,5-dichloro-1-hydroxypyridin-4-imine 91872-02-5 C5H4Cl2N2O
3,5-dichloro-1-hydroxypyridin-4-imine
—— 3-(4-trifluoromethylphenyl)prop-2-yn-1-ol 173546-21-9 C10H7F3O
3-(4-trifluoromethylphenyl)prop-2-yn-1-ol
—— 2-((10S,13S,17R)-17-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,10,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate 7753-60-8 C23H30O5
2-((10S,13S,17R)-17-hydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,10,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate
—— tert-butyl (S)-3-(4-aminophenyl)piperidine-1-carboxylate 1171197-20-8 C16H24N2O2
tert-butyl (S)-3-(4-aminophenyl)piperidine-1-carboxylate
—— lovastatin hydroxy acid sodium salt 75225-50-2 C24H37O6*Na
lovastatin hydroxy acid sodium salt
—— (1S,5R)-1-(3-fluorophenyl)-3-oxabicyclo[3.1.0]hexan-2-one 528587-70-4 C11H9FO2
(1S,5R)-1-(3-fluorophenyl)-3-oxabicyclo[3.1.0]hexan-2-one
—— ((1R,2S)-2-(3-fluorophenyl)-2-(hydroxymethyl)cyclopropyl)methyl acetate 1369768-29-5 C13H15FO3
((1R,2S)-2-(3-fluorophenyl)-2-(hydroxymethyl)cyclopropyl)methyl acetate
—— SM-04554 1360540-81-3 C18H16O4
SM-04554
—— atorvastatin sodium 134523-01-6 C33H34FN2O5*Na
atorvastatin sodium
—— 1,4,7,10-tetrakis(2-pyridylmethyl)-1,4,7,10-tetraazacyclododecane 185130-32-9 C32H40N8
1,4,7,10-tetrakis(2-pyridylmethyl)-1,4,7,10-tetraazacyclododecane
—— sarolaner 1398609-39-6 C23H18Cl2F4N2O5S
sarolaner
—— (1S,3R,3'S)-bis(tert-butyldimethylsilyloxy)-20(R)-(3'-cyclopropyl-3'-hydroxyprop-1'(E)-enyl)-9,10-secopregna-5(E),7(E),10(19)-triene 112849-27-1 C39H68O3Si2
(1S,3R,3'S)-bis(tert-butyldimethylsilyloxy)-20(R)-(3'-cyclopropyl-3'-hydroxyprop-1'(E)-enyl)-9,10-secopregna-5(E),7(E),10(19)-triene
—— formamidine disulfide dihydrochloride 14807-75-1 C2H6N4S2*2ClH
formamidine disulfide dihydrochloride
—— 2-amino-6-isopropylpyrimidin-4-ol 73576-32-6 C7H11N3O
2-amino-6-isopropylpyrimidin-4-ol
—— 6-(3-bromo-5-methyl-benzoyl)-5-isopropyl-1H-pyrimidine-2,4-dione 1006300-03-3 C15H15BrN2O3
6-(3-bromo-5-methyl-benzoyl)-5-isopropyl-1H-pyrimidine-2,4-dione
—— 2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetic acid 82152-06-5 C9H7NO3S
2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetic acid
—— 7-bromo-4-fluoro-1-benzothiophene 324768-96-9 C8H4BrFS
7-bromo-4-fluoro-1-benzothiophene
—— (E)-2-chloro-3-(hydroxymethylene)cyclohex-1-ene-1-carbaldehyde 1416808-92-8 C8H9ClO2
(E)-2-chloro-3-(hydroxymethylene)cyclohex-1-ene-1-carbaldehyde
—— 2-fluoro-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzonitrile 1029714-87-1 C22H13FN6
2-fluoro-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzonitrile
—— 9,9'-(biphenyl-4,4'-diyl)bis(fluoren-9-ol) 427165-44-4 C38H26O2
9,9'-(biphenyl-4,4'-diyl)bis(fluoren-9-ol)
—— 3-benzyladenine 7280-81-1 C12H11N5
3-benzyladenine
—— methyl 6-bromo-2,3-difluorobenzoate 364727-87-7 C8H5BrF2O2
methyl 6-bromo-2,3-difluorobenzoate
—— (2',4''-O-bistrimethylsilyl)-6-O-methylerythromycinA-9[O-(1-ethoxy-1-methylethyl)]oxime 119665-62-2 C49H96N2O14Si2
(2',4''-O-bistrimethylsilyl)-6-O-methylerythromycinA-9[O-(1-ethoxy-1-methylethyl)]oxime
—— 1-hydroxy-4-(5-pyridin-4-yl-1,2,4-triazol-3-ylidene)pyridine 36770-53-3 C12H9N5O
1-hydroxy-4-(5-pyridin-4-yl-1,2,4-triazol-3-ylidene)pyridine
—— enmetazobactam 1001404-83-6 C11H14N4O5S
enmetazobactam
—— 6-chloro-1,7-naphthyridin-4-ol 1214241-98-1 C8H5ClN2O
6-chloro-1,7-naphthyridin-4-ol
—— sodium taurochenodeoxycholate 6009-98-9 C26H44NO6S*Na
sodium taurochenodeoxycholate
—— (2S,5S)-tert-butyl 5-hydroxypiperidine-2-carboxylate 1383814-52-5 C10H19NO3
(2S,5S)-tert-butyl 5-hydroxypiperidine-2-carboxylate
—— 3-amino-4-(2,4,5-trifluorophenyl)butanoic acid 1283583-85-6 C10H10F3NO2
3-amino-4-(2,4,5-trifluorophenyl)butanoic acid
—— 5-Hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde 60484-29-9 C11H10N2O2
5-Hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde
—— 1-chloroethyl sulfochloridate 90906-61-9 C2H4Cl2O3S
1-chloroethyl sulfochloridate
—— 2-naphthylmethyl acrylate 93359-80-9 C14H12O2
2-naphthylmethyl acrylate
—— (E)-2-styrylpyridin-3-amine 209798-50-5 C13H12N2
(E)-2-styrylpyridin-3-amine
—— (R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 1022150-12-4 C22H22N6O
(R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
—— 2-(pyridine-2-yliminomethyl)phenol 1823-47-8 C12H10N2O
2-(pyridine-2-yliminomethyl)phenol
—— 7-amino-3-[(1H-1-methyltetrazole-5-yl)thio]methylceph-3-em-4-carboxylic acid 24209-38-9 C10H12N6O3S2
7-amino-3-[(1H-1-methyltetrazole-5-yl)thio]methylceph-3-em-4-carboxylic acid
—— vitamin K<sub>1</sub> 2,3 epoxide 25486-55-9 C31H46O3
vitamin K<sub>1</sub> 2,3 epoxide
—— 1-acetyl-3-[(Z)-benzylidene]-2,5-piperazinedione 30166-29-1 C13H12N2O3
1-acetyl-3-[(Z)-benzylidene]-2,5-piperazinedione
—— 3-aminoquinuclidine dihydrochloride 6530-09-2 C7H14N2*2ClH
3-aminoquinuclidine dihydrochloride
—— 1,3-dimethylvioluric acid 5417-13-0 C6H7N3O4
1,3-dimethylvioluric acid