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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
—— 5-methylsulfanyl-1<i>H</i>-pyrimidine-2,4-dione 16350-59-7 C5H6N2O2S
5-methylsulfanyl-1<i>H</i>-pyrimidine-2,4-dione
—— 1-(4-methoxy-2-methylphenyl)-2-methyl-1H-imidazo[4,5-c]pyridine 1609259-89-3 C15H15N3O
1-(4-methoxy-2-methylphenyl)-2-methyl-1H-imidazo[4,5-c]pyridine
—— uvitonic acid 499-50-3 C8H7NO4
uvitonic acid
—— Geranyl arabinopyranosyl-glucoside 150995-11-2 C21H36O10
Geranyl arabinopyranosyl-glucoside
—— 1,3-dichloro-2-fluoro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene 928783-84-0 C9H4Cl2F4
1,3-dichloro-2-fluoro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene
—— 5,6-Difluoro-benzofuran-2-carboxylic acid 199287-53-1 C9H4F2O3
5,6-Difluoro-benzofuran-2-carboxylic acid
—— 4-ethoxycarbonylmethylcyclohexanecarboxylic acid 193903-32-1 C11H18O4
4-ethoxycarbonylmethylcyclohexanecarboxylic acid
—— 6-chloro-2,7-dimethyl-imidazo[1,2-b]pyridazine 17412-20-3 C8H8ClN3
6-chloro-2,7-dimethyl-imidazo[1,2-b]pyridazine
—— methyl 4-isocyanatosulfonyl-5-methylthiophene-3-carboxylate 897671-34-0 C8H7NO5S2
methyl 4-isocyanatosulfonyl-5-methylthiophene-3-carboxylate
—— 5-methylisatin-3-oxime 13208-98-5 C9H8N2O2
5-methylisatin-3-oxime
—— Encequidar Mesylate 849675-87-2 C39H42N6O11S
Encequidar Mesylate
—— Quinoline-2-carbothioamide 96898-30-5 C10H8N2S
Quinoline-2-carbothioamide
—— 1-Isoproxypropyl-1,2-dihydro-6-hydroxy-4-methyl-2-oxo-3-pyridinecarbonitrile 68612-94-2 C13H18N2O3
1-Isoproxypropyl-1,2-dihydro-6-hydroxy-4-methyl-2-oxo-3-pyridinecarbonitrile
—— 1-benzyl-4-p-tolyl-1,2,3,6-tetrahydro-pyridine 13314-67-5 C19H21N
1-benzyl-4-p-tolyl-1,2,3,6-tetrahydro-pyridine
—— 6-chloro-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl 439215-13-1 C11H11ClN2
6-chloro-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl
—— 83766-73-8 C12H24NaO5S
—— cis-4-methoxycyclohexanol 22188-02-9 C7H14O2
cis-4-methoxycyclohexanol
—— 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-carboxylic acid hydrochloride 1156899-12-5 C12H12N2O2*ClH
2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-carboxylic acid hydrochloride
—— 6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazin-2-amine 1333508-93-2 C6H9N3O
6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazin-2-amine
—— ethyl 7-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate 1380331-36-1 C9H8BrN3O2
ethyl 7-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate
—— N-tert-butyloxanillic acid ethyl ester 87034-69-3 C8H15NO3
N-tert-butyloxanillic acid ethyl ester
—— bicyclo<3.1.1>heptane-1,5-dicarboxylic acid 75328-55-1 C9H12O4
bicyclo<3.1.1>heptane-1,5-dicarboxylic acid
—— 6-bromo-8-methyl-2(1H)-quinolinone 99465-08-4 C10H8BrNO
6-bromo-8-methyl-2(1H)-quinolinone
—— 1,1-Dicyan-4-(N,N-dimethylamino)-2-methoxybutadien-1,3 95689-38-6 C9H11N3O
1,1-Dicyan-4-(N,N-dimethylamino)-2-methoxybutadien-1,3
—— methyl 2-(5-bromo-1H-indol-3-yl)-2-oxoacetate 163160-56-3 C11H8BrNO3
methyl 2-(5-bromo-1H-indol-3-yl)-2-oxoacetate
—— 6-nitro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one 55727-50-9 C11H9N3O3
6-nitro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
—— 3,3'-(3-fluorobenzylidene)bis(4-hydroxycoumarin) 6160-02-7 C25H15FO6
3,3'-(3-fluorobenzylidene)bis(4-hydroxycoumarin)
—— N,N-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine 1321518-05-1 C13H21BN2O2
N,N-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine
—— JA2131 6505-99-3 C13H19N5O2S2
JA2131
—— 3-pyridylphenolate sodium salt 52536-09-1 C5H4NO*Na
3-pyridylphenolate sodium salt
—— phenyl N-benzyl-2-amino-4,6-O-benzylidene-2,3-N,O-carbonyl-2-deoxy-1-thio-β-D-glucopyranoside 910805-49-1 C27H25NO5S
phenyl N-benzyl-2-amino-4,6-O-benzylidene-2,3-N,O-carbonyl-2-deoxy-1-thio-β-D-glucopyranoside
—— endo-methyl-norbornene-5-carboxylate 6203-08-3 C9H12O2
endo-methyl-norbornene-5-carboxylate
—— sodium pyrimidine-5-carboxylate 352535-06-9 C5H3N2O2*Na
sodium pyrimidine-5-carboxylate
—— 3,5-di(pyridin-2-yl)-1,2,4-triazole 1671-85-8 C12H9N5
3,5-di(pyridin-2-yl)-1,2,4-triazole
—— 6-bromo-1,5-dimethylpyrimidine-2,4(1H,3H)-dione 1609259-61-1 C6H7BrN2O2
6-bromo-1,5-dimethylpyrimidine-2,4(1H,3H)-dione
—— methyl 6-bromo-1-methyl-1H-indole-3-carboxylate 946427-09-4 C11H10BrNO2
methyl 6-bromo-1-methyl-1H-indole-3-carboxylate
—— 8-bromotetrazolo[1,5-a]pyridine 54230-88-5 C5H3BrN4
8-bromotetrazolo[1,5-a]pyridine
—— ethyl 2-cyclopropyl-2-hydroxyacetate 1185387-66-9 C7H12O3
ethyl 2-cyclopropyl-2-hydroxyacetate
—— Pyrimidin-aldehyd-(4)-oxim 1073-65-0 C5H5N3O
Pyrimidin-aldehyd-(4)-oxim
—— 5-methyl-1<i>H</i>-pyrimidine-4,6-dione 63447-38-1 C5H6N2O2
5-methyl-1<i>H</i>-pyrimidine-4,6-dione
—— 6-hydroxy-2-methylpyrimidine-4-carboxylic acid 34415-10-6 C6H6N2O3
6-hydroxy-2-methylpyrimidine-4-carboxylic acid
—— 5-(trifluoromethyl)pyrimidine 69034-12-4 C5H3F3N2
5-(trifluoromethyl)pyrimidine
—— 4-hydroxy-6-methylpyrimidine-5-carboxylic acid ethyl ester 157981-55-0 C8H10N2O3
4-hydroxy-6-methylpyrimidine-5-carboxylic acid ethyl ester
—— N-(cyclohexyl)-4-bromonaphthalene-1,8-dicarboxiimide 324035-44-1 C18H16BrNO2
N-(cyclohexyl)-4-bromonaphthalene-1,8-dicarboxiimide
—— (R)-4-[(1-Methylheptyloxy)carbonyl]phenyl 4'-octyloxy-4-biphenylcarboxylate 123286-51-1 C36H46O5
(R)-4-[(1-Methylheptyloxy)carbonyl]phenyl 4'-octyloxy-4-biphenylcarboxylate
—— 2,6-di(3-methylpyrazol-1-yl)pyridine 853748-46-6 C13H13N5
2,6-di(3-methylpyrazol-1-yl)pyridine
—— 1-hydroxy-1-benzoylcyclopentane 19300-92-6 C12H14O2
1-hydroxy-1-benzoylcyclopentane
—— ethyl 2-cyano-2-(dihydro-2H-pyran-4(3H)-ylidene)acetate 33451-54-6 C10H13NO3
ethyl 2-cyano-2-(dihydro-2H-pyran-4(3H)-ylidene)acetate
—— tri(4-pyridyl)phosphane 94345-03-6 C15H12N3P
tri(4-pyridyl)phosphane
—— 6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridine-3-carbonitrile 57663-05-5 C8H8N2OS
6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridine-3-carbonitrile