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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
—— methanesulfonic acid 2-[2-methyl-5-(4-methylsulfanylphenyl)pyrrol-1-yl]ethyl ester 494850-87-2 C15H19NO3S2
methanesulfonic acid 2-[2-methyl-5-(4-methylsulfanylphenyl)pyrrol-1-yl]ethyl ester
—— 6-hydroxy-2-methyl-2H-pyran-3(6H)-one 41728-14-7 C6H8O3
6-hydroxy-2-methyl-2H-pyran-3(6H)-one
—— 3-(6-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione 1416990-09-4 C13H12N2O4
3-(6-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione
—— 2,2'-dibromo-4,4'-bis(2-ethylhexyl)[6,6'-bithieno[3,2,b]pyrrolylidene]-5,5'(4H,4H')-dione 1147124-49-9 C28H36Br2N2O2S2
2,2'-dibromo-4,4'-bis(2-ethylhexyl)[6,6'-bithieno[3,2,b]pyrrolylidene]-5,5'(4H,4H')-dione
—— 2-bromoethyltetrahydropyranylether 172797-67-0 C7H13BrO2
2-bromoethyltetrahydropyranylether
—— 1-<2-(3,4-Dimethoxyphenyl)ethyl>pyrimidin-2,4,6(1H,3H,5H)-trion 75535-95-4 C14H16N2O5
1-<2-(3,4-Dimethoxyphenyl)ethyl>pyrimidin-2,4,6(1H,3H,5H)-trion
—— 2,3,6,7,10,11-hexamethyldipyrazino<2,3-f;2',3'-h>quinoxaline 96355-60-1 C18H18N6
2,3,6,7,10,11-hexamethyldipyrazino<2,3-f;2',3'-h>quinoxaline
—— 7-bromopyrido[3,2-d]pyrimidin-4(3H)-one 573675-29-3 C7H4BrN3O
7-bromopyrido[3,2-d]pyrimidin-4(3H)-one
—— 2-amino-5-iodo-3-chlorobenzoic acid 101012-31-1 C7H5ClINO2
2-amino-5-iodo-3-chlorobenzoic acid
—— 2,5-dibromo-3-(methylthio)thiophene 94781-42-7 C5H4Br2S2
2,5-dibromo-3-(methylthio)thiophene
—— 3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)-acrylic acid 133262-97-2 C17H15ClO4
3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)-acrylic acid
—— 3-mercapto-2-ethoxycarbonylthiophene 1027291-35-5 C7H8O2S2
3-mercapto-2-ethoxycarbonylthiophene
—— 5-chloro-2-fluoro-N-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)phenyl]benzenesulfonamide 1428182-88-0 C18H20BClFNO4S
5-chloro-2-fluoro-N-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)phenyl]benzenesulfonamide
—— 2,4-dimethyl-3-butylpyrrole 151464-91-4 C10H17N
2,4-dimethyl-3-butylpyrrole
—— Erythromycin, 9-oxime 13127-18-9 C37H68N2O13
Erythromycin, 9-oxime
—— 4′-(2,4-dimethoxyphenyl)-2,2′:6′,2″-terpyridine 1239020-51-9 C23H19N3O2
4′-(2,4-dimethoxyphenyl)-2,2′:6′,2″-terpyridine
—— 6-chloro-5-methoxy-3-methylindole 172170-01-3 C10H10ClNO
6-chloro-5-methoxy-3-methylindole
—— Pregnenolon-3β-sulfonsaeureester 1247-64-9 C21H32O5S
Pregnenolon-3β-sulfonsaeureester
—— Pregnenolon-sulfat 1247-64-9 C21H32O5S
Pregnenolon-sulfat
—— 5-(4-fluorophenyl)pyrrolidin-2-one 90432-58-9 C10H10FNO
5-(4-fluorophenyl)pyrrolidin-2-one
—— Cis-di-tert-butyl-cyclopent-4-ene-1,3-diyl dicarbonate 890122-43-7 C15H24O6
Cis-di-tert-butyl-cyclopent-4-ene-1,3-diyl dicarbonate
—— 2-phenoxycyclopropane carboxylic acid 7252-94-0 C10H10O3
2-phenoxycyclopropane carboxylic acid
—— 3-(5-hydroxypyrimidin-2-yl)benzoic acid 1092568-86-9 C11H8N2O3
3-(5-hydroxypyrimidin-2-yl)benzoic acid
—— 17β-cyano-3,3-[1,2-ethanediylbis(oxy)]-17α-trimethylsilyloxyestra-5(10),9(11)-diene 54690-63-0 C24H35NO3Si
17β-cyano-3,3-[1,2-ethanediylbis(oxy)]-17α-trimethylsilyloxyestra-5(10),9(11)-diene
—— (3S)-Boc-amino-(4R)-ethyl-piperidine 488728-05-8 C12H24N2O2
(3S)-Boc-amino-(4R)-ethyl-piperidine
—— (2S)-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]pent-4-enoic acid 136092-76-7 C11H19NO4
(2S)-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]pent-4-enoic acid
—— ethyl [4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate 1260543-99-4 C12H17N3O4
ethyl [4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate
—— 1-(5-cyanopyridin-2-yl)piperidine-4-carboxylic acid 162997-28-6 C12H13N3O2
1-(5-cyanopyridin-2-yl)piperidine-4-carboxylic acid
—— 5-chloro-2,3-dihydro-4(1H)-quinolinone 21617-16-3 C9H8ClNO
5-chloro-2,3-dihydro-4(1H)-quinolinone
—— N-(5-amino-2-chloro-4-fluoro-benzoyl)-N'-methyl-N'-isopropylsulfamide 685568-49-4 C11H15ClFN3O3S
N-(5-amino-2-chloro-4-fluoro-benzoyl)-N'-methyl-N'-isopropylsulfamide
—— N,N,N',N'-Tetramethylpiperazinium diiodide 6952-20-1 C8H20N2*2I
N,N,N',N'-Tetramethylpiperazinium diiodide
—— (2,2-diphenyltetrahydrofuran-3-yl)methanol 93651-75-3 C17H18O2
(2,2-diphenyltetrahydrofuran-3-yl)methanol
—— 8-bromo-5-chloro-[1,2,4]-triazolo[1,5-a]pyridine 1030626-87-9 C6H3BrClN3
8-bromo-5-chloro-[1,2,4]-triazolo[1,5-a]pyridine
—— MIND4-19 129544-85-0 C22H19N3OS
MIND4-19
—— ethyl 3-amino-5-bromopyridine-2-carboxylate 1334405-60-5 C8H9BrN2O2
ethyl 3-amino-5-bromopyridine-2-carboxylate
—— 6-bromo-2-methoxy-3-methyl-quinoline 854524-01-9 C11H10BrNO
6-bromo-2-methoxy-3-methyl-quinoline
—— 2-phenyl-[1,6]naphthyridine 52816-59-8 C14H10N2
2-phenyl-[1,6]naphthyridine
—— phenyl-di-[2]pyridyl-phosphine sulfide 165612-56-6 C16H13N2PS
phenyl-di-[2]pyridyl-phosphine sulfide
—— 2-methyl-7-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylic acid 1032267-56-3 C10H11NO3
2-methyl-7-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylic acid
—— Adavelt 1961312-55-9 C27H26F2N2O6
Adavelt
—— methyl 5-hydroxypyrazolo[1,5-a]pyridine-3-carboxylate 1060724-74-4 C9H8N2O3
methyl 5-hydroxypyrazolo[1,5-a]pyridine-3-carboxylate
—— 4-hydroxy-2-oxo-2H-coumarin-3-yl styryl ketone 209973-90-0 C18H12O4
4-hydroxy-2-oxo-2H-coumarin-3-yl styryl ketone
—— 2-propenamide, N-[2-hydroxy-2-(4-methoxyphenyl)ethyl]-3-phenyl-, (2E) 456-12-2 C18H19NO3
2-propenamide, N-[2-hydroxy-2-(4-methoxyphenyl)ethyl]-3-phenyl-, (2E)
—— 3-(5-bromothiophen-2-yl)-2,5-bis(2-hexyldecyl)-6-(thiophen-2-yl)pyrrolo[3,4-c]pyrrole-1,4(2H,5H)-dione 1423138-95-7 C46H71BrN2O2S2
3-(5-bromothiophen-2-yl)-2,5-bis(2-hexyldecyl)-6-(thiophen-2-yl)pyrrolo[3,4-c]pyrrole-1,4(2H,5H)-dione
—— N'-(5-fluoro-2-oxoindolin-3-ylidene)-4-hydroxybenzohydrazide 330572-32-2 C15H10FN3O3
N'-(5-fluoro-2-oxoindolin-3-ylidene)-4-hydroxybenzohydrazide
—— 4-methoxy-dibenzofuran-1-ylamine 685873-83-0 C13H11NO2
4-methoxy-dibenzofuran-1-ylamine
—— AZ7550 1421373-99-0 C27H31N7O2
AZ7550
—— 4-mesitylaniline 66818-61-9 C15H17N
4-mesitylaniline
—— 5-fluorobarbituric acid 767-80-6 C4H3FN2O3
5-fluorobarbituric acid
—— 1-(3-chloropropyl)pyridinium bromide 76892-41-6 Br*C8H11ClN
1-(3-chloropropyl)pyridinium bromide