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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
—— 1'-([5-(aminomethyl)-1-(4,4,4-trifluorobutyl)-1H-1,3-benzodiazol-2-yl]methyl)-6'-fluoro-1',2'-dihydrospiro[cyclopropane-1,3'-indole]-2'-one 1903763-82-5 C23H22F4N4O
1'-([5-(aminomethyl)-1-(4,4,4-trifluorobutyl)-1H-1,3-benzodiazol-2-yl]methyl)-6'-fluoro-1',2'-dihydrospiro[cyclopropane-1,3'-indole]-2'-one
—— 7-tert-butyl 6-hydrogen (1R,5S,6S)-3,3-dimethyl-2,4-dioxa-7-azabicyclo<3.3.0>octane-6,7-dicarboxylate 127910-62-7 C13H21NO6
7-tert-butyl 6-hydrogen (1R,5S,6S)-3,3-dimethyl-2,4-dioxa-7-azabicyclo<3.3.0>octane-6,7-dicarboxylate
—— (2,6-dichloro-phenyl)-pyrimidin-2-yl-amine 66501-16-4 C10H7Cl2N3
(2,6-dichloro-phenyl)-pyrimidin-2-yl-amine
—— 2,6-bis(3-isopropylphenyl)benzaldehyde 934334-00-6 C25H26O
2,6-bis(3-isopropylphenyl)benzaldehyde
—— 3-(3-carboxypropyl)-7-sulfomethyl-1H-indole-2-carboxylic acid ethyl ester 860398-31-8 C16H19NO7S
3-(3-carboxypropyl)-7-sulfomethyl-1H-indole-2-carboxylic acid ethyl ester
—— 1-(6-bromo-pyridin-2-yl)-3-carboethoxy-thiourea 1010120-59-8 C9H10BrN3O2S
1-(6-bromo-pyridin-2-yl)-3-carboethoxy-thiourea
—— 4-methyl-4,7-diazaspiro[2.5]octane 1152367-88-8 C7H14N2
4-methyl-4,7-diazaspiro[2.5]octane
—— N-[(2-fluorophenyl)methylideneamino]-4-methoxy-6-piperidin-1-yl-1,3,5-triazin-2-amine 5866-56-8 C16H19FN6O
N-[(2-fluorophenyl)methylideneamino]-4-methoxy-6-piperidin-1-yl-1,3,5-triazin-2-amine
—— Disodium 4,5-dihydro-5-oxo-4-(phenylazo)-1-(4-sulphonatophenyl)-1H-pyrazole-3-carboxylate 1934-22-1 C16H10N4Na2O6S
Disodium 4,5-dihydro-5-oxo-4-(phenylazo)-1-(4-sulphonatophenyl)-1H-pyrazole-3-carboxylate
—— Disodium 4,5-dihydro-5-oxo-1-(4-sulfophenyl)-1H-pyrazole-3-carboxylate 3473-75-4 C10H6N2Na2O6S
Disodium 4,5-dihydro-5-oxo-1-(4-sulfophenyl)-1H-pyrazole-3-carboxylate
—— 5-tert-butylbenzo<b>thiophene-2-carboxylic acid 126231-21-8 C13H14O2S
5-tert-butylbenzo<b>thiophene-2-carboxylic acid
—— 7-bromo-5-methoxyindole 408355-12-4 C9H8BrNO
7-bromo-5-methoxyindole
—— vimseltinib 1628606-05-2 C23H25N7O2
vimseltinib
—— Cholesterylsulfat 1256-86-6 C27H46O4S
Cholesterylsulfat
—— 2-[Carbamoyl-[(5-nitrofuran-2-yl)methylideneamino]amino]acetic acid 63981-22-6 C8H8N4O6
2-[Carbamoyl-[(5-nitrofuran-2-yl)methylideneamino]amino]acetic acid
—— tert-butyl (S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylate 103733-66-0 C16H23NO4
tert-butyl (S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
—— 4-bromo-1-(4-methoxyphenyl)-1H-pyrazole 1215007-02-5 C10H9BrN2O
4-bromo-1-(4-methoxyphenyl)-1H-pyrazole
—— 1-(2,4-dihydroxyphenyl)-3-(4-methylphenyl) propenone 36574-88-6 C16H14O3
1-(2,4-dihydroxyphenyl)-3-(4-methylphenyl) propenone
—— 5-aminoindoline dihydrochloride 2759-14-0 C8H10N2*2ClH
5-aminoindoline dihydrochloride
—— methyl 7-bromo-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-5-carboxylate 1301214-77-6 C9H7BrN2O3
methyl 7-bromo-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-5-carboxylate
—— (+/-)-(9a<i>r</i>)-octahydro-quinolizin-3<i>c</i>-carboxylic acid ethyl ester 19728-76-8 C12H21NO2
(+/-)-(9a<i>r</i>)-octahydro-quinolizin-3<i>c</i>-carboxylic acid ethyl ester
—— (2S,5R)-7-oxo-N-[(4R)-azepan-4-yl]-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide 1174019-01-2 C13H22N4O6S
(2S,5R)-7-oxo-N-[(4R)-azepan-4-yl]-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide
—— (6-Bromo-2-oxo-benzooxazol-3-yl)-acetic acid 100219-71-4 C9H6BrNO4
(6-Bromo-2-oxo-benzooxazol-3-yl)-acetic acid
—— (R)-4-benzyl-2-(pyridin-2-yl)-4,5-dihydrooxazole 108915-08-8 C15H14N2O
(R)-4-benzyl-2-(pyridin-2-yl)-4,5-dihydrooxazole
—— 4-vinylpyridine cation 100-43-6 C7H7N
4-vinylpyridine cation
—— BMS-262084 253174-92-4 C18H31N7O5
BMS-262084
—— 7-chloro-1,3-dihydro-imidazo[4,5-b]pyridin-2-one 1202780-76-4 C6H4ClN3O
7-chloro-1,3-dihydro-imidazo[4,5-b]pyridin-2-one
—— 6-Methylergoline-8-carboxylic acid 5878-43-3 C16H18N2O2
6-Methylergoline-8-carboxylic acid
—— 17-Cyano-9,17-dihydroxyandrost-4-ene-3-one 116256-35-0 C20H27NO3
17-Cyano-9,17-dihydroxyandrost-4-ene-3-one
—— 4-Ammonio-1-benzylpiperidinium dichloride 1205-72-7 C12H18ClN2-
4-Ammonio-1-benzylpiperidinium dichloride
—— 2-Chloro-1-methylpyridinium toluene-p-sulphonate 7403-46-5 C13H15ClNO3S+
2-Chloro-1-methylpyridinium toluene-p-sulphonate
—— (1S-(1alpha,3Abeta,4alpha,8abeta,9R*))-decahydro-4,8,8-trimethyl-1,4-methanoazulene-9-methanol 1139-17-9 C15H26O
(1S-(1alpha,3Abeta,4alpha,8abeta,9R*))-decahydro-4,8,8-trimethyl-1,4-methanoazulene-9-methanol
—— 4-(Dimethylammonio)piperidinium dichloride 4876-59-9 C7H16ClN2-
4-(Dimethylammonio)piperidinium dichloride
—— 4-Methylpyrimidine-2-thiol HCl 6959-66-6 C5H6ClN2S-
4-Methylpyrimidine-2-thiol HCl
—— Einecs 254-166-6 38869-47-5 C11H16ClN2O-
Einecs 254-166-6
—— (8alpha,9R)-1-Benzyl-9-hydroxycinchonanium chloride 69257-04-1 C26H30ClN2O+
(8alpha,9R)-1-Benzyl-9-hydroxycinchonanium chloride
—— Pyrimidine-4,6-diammonium hydrogen sulphate (1:2) 77709-02-5 C4H8N4O
Pyrimidine-4,6-diammonium hydrogen sulphate (1:2)
—— Cinchonidine sulfate dihydrate 524-61-8 C38H50N4O8S
Cinchonidine sulfate dihydrate
—— (1S,2R,4S,5R)-1-Benzyl-2-(hydroxy(quinolin-4-yl)methyl)-5-vinylquinuclidin-1-ium chloride 69221-14-3 C26H29ClN2O
(1S,2R,4S,5R)-1-Benzyl-2-(hydroxy(quinolin-4-yl)methyl)-5-vinylquinuclidin-1-ium chloride
—— 8-Azepan-2-YL-quinoline 527673-84-3 C15H18N2
8-Azepan-2-YL-quinoline
—— 5-Bromo-2,3-dihydro-3,3-dimethylbenzofuran-2-one 75097-60-8 C10H9BrO2
5-Bromo-2,3-dihydro-3,3-dimethylbenzofuran-2-one
—— 5-chloro-[1,2,4]triazolo[1,5-a]pyrazin-2-ylamine 1454653-85-0 C5H4ClN5
5-chloro-[1,2,4]triazolo[1,5-a]pyrazin-2-ylamine
—— Ethyl 2-Methylthioindolizine-3-carboxylate 123471-45-4 C12H13NO2S
Ethyl 2-Methylthioindolizine-3-carboxylate
—— chloro(2-dicyclohexylphosphino-2',6'-dimethoxy-1,1'-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) 1028206-58-7 C34H45ClNO2PPd
chloro(2-dicyclohexylphosphino-2',6'-dimethoxy-1,1'-biphenyl)[2-(2-aminoethylphenyl)]palladium(II)
—— 5-Bromo-N-(pyridin-4-YL)pyrimidin-2-amine 887433-72-9 C9H7BrN4
5-Bromo-N-(pyridin-4-YL)pyrimidin-2-amine
—— 2-Imino-4-nitropyridin-1(2H)-ol 52092-45-2 C5H5N3O3
2-Imino-4-nitropyridin-1(2H)-ol
—— Calcium 4-methyl-2-oxovalerate 51828-95-6 C12H18CaO6
Calcium 4-methyl-2-oxovalerate
—— ethyl 2-amino-3-pyridineacrylate 104830-07-1 C10H12N2O2
ethyl 2-amino-3-pyridineacrylate
—— N,N'-diphenylethane-1,2-diimine 30834-75-4 C14H12N2
N,N'-diphenylethane-1,2-diimine
—— 5-Azepan-2-YL-quinoline 527673-86-5 C15H18N2
5-Azepan-2-YL-quinoline