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原料药中间体

原料药中间体是指在药物合成过程中用于生成最终活性成分(即原料药)的化学物质。这些中间体在制药工业中扮演着重要角色,它们通过一系列化学反应逐步转化成成品药物。根据其在生产过程中的位置和功能,可以将原料药中间体分为以下几个类别:

  1. 起始物料:这类中间体是最初用于合成最终产品的原材料。它们通常来源于天然产物、化工产品或其他已经存在的化合物。

  2. 关键中间体:这些中间体在整个合成过程中起着核心作用,通常是通过复杂的化学反应得到的。它们对于确保原料药的质量和成本效益至关重要。

  3. 保护基团:在药物合成中使用这类中间体是为了对某些敏感部分进行临时性或选择性的“保护”,防止它们在不必要的位置上发生副反应。保护完成后可通过特定条件去除这些保护基。

  4. 催化剂和添加剂:虽然不直接形成最终产品,但这些物质能够促进化学反应、提高产率或改善产品的质量特性。

  5. 分离纯化溶剂:这类中间体主要用于原料药合成过程中的提纯步骤。它们帮助从目标产物中去除杂质并提高产品的纯度。

选择合适的原料药中间体对于保证药物的安全性和有效性至关重要,因此,在其开发过程中需要考虑多个因素,包括成本效益、反应条件的可控性以及环境友好型等方面。

下级分类

中文名称 英文名称 CAS号 化学式 结构式图片
—— Norcarane-3-amine, hydrochloride 78293-49-9 C7H14ClN
Norcarane-3-amine, hydrochloride
—— BMS-262084 253174-92-4 C18H31N7O5
BMS-262084
—— trans-2-trifluoromethylcyclopropylmethanol 22666-34-8 C5H7F3O
trans-2-trifluoromethylcyclopropylmethanol
—— 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-(Dimethylammonio)piperidinium dichloride 4876-59-9 C7H16ClN2-
4-(Dimethylammonio)piperidinium dichloride
—— Einecs 254-166-6 38869-47-5 C11H16ClN2O-
Einecs 254-166-6
—— Fosfomycin (R)-1-phenethylamine monohydrate 65794-75-4 C3H7O4P*C8H11N*H2O
Fosfomycin (R)-1-phenethylamine monohydrate
—— Gallium Ga-68 gozetotide 1366302-52-4 C44H59GaN6O17
Gallium Ga-68 gozetotide
—— Difelikefalin Acetate 1024829-44-4 C38H57N7O8
Difelikefalin Acetate
—— 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)
—— Fluticasone 17beta-Carboxylic Acid 1174462-25-9 C21H26F2O5
Fluticasone 17beta-Carboxylic Acid
—— cis-Ethyl 3-aminocyclobutanecarboxylate hydrochloride 957793-35-0 C7H13NO2*ClH
cis-Ethyl 3-aminocyclobutanecarboxylate hydrochloride
—— tabernaemontanine 2134-98-7 C21H26N2O3
tabernaemontanine
—— 3,3-Difluorocyclohexane-1-carbonitrile 1227808-14-1 C7H9F2N
3,3-Difluorocyclohexane-1-carbonitrile
—— 4-aminopiperidine-1,4-dicarboxylic acid-1-tert-butyl ester-4-ethyl ester 1187321-32-9 C13H24N2O4
4-aminopiperidine-1,4-dicarboxylic acid-1-tert-butyl ester-4-ethyl ester
—— Δ<sup>3,5</sup>-Androstadien-3,17-dion 1420-49-1 C19H24O2
Δ<sup>3,5</sup>-Androstadien-3,17-dion
—— Morellin 1183-12-6 C33H36O7
Morellin
—— D-(+)-3-Bromocamphor 10293-06-8 C10H15BrO
D-(+)-3-Bromocamphor
—— 2-(5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-5-(phenylazo)pyrimidine-4,6-diamine 1350653-29-0 C23H17F2N9
2-(5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)-5-(phenylazo)pyrimidine-4,6-diamine
—— methyl (2S,3S)-2-(tert-butoxycarbonyl)amino-3-hydroxy-3-phenylpropionate 17193-36-1 C15H21NO5
methyl (2S,3S)-2-(tert-butoxycarbonyl)amino-3-hydroxy-3-phenylpropionate
—— 18-(2-Carboxyethyl)-20-(carboxymethyl)-12-ethenyl-7-ethyl-3,8,13,17-tetramethyl-17,18,22,23-tetrahydroporphyrin-2-carboxylic acid 19660-77-6 C34H36N4O6
18-(2-Carboxyethyl)-20-(carboxymethyl)-12-ethenyl-7-ethyl-3,8,13,17-tetramethyl-17,18,22,23-tetrahydroporphyrin-2-carboxylic acid
—— Isomorellin 1183-12-6 C33H36O7
Isomorellin
—— Chlorin e6 19660-77-6 C34H36N4O6
Chlorin e6
—— 5-bromopyrazolo[1,5-a]pyridine-3-carbonitrile 1352900-95-8 C8H4BrN3
5-bromopyrazolo[1,5-a]pyridine-3-carbonitrile
—— bicyclo[4.1.0]heptane-3-carboxylic acid 710314-32-2 C8H12O2
bicyclo[4.1.0]heptane-3-carboxylic acid
—— 1-butyl-2-methylbenzo[cd]indol-1-ium iodide 1151666-46-4 C16H18N*I
1-butyl-2-methylbenzo[cd]indol-1-ium iodide
—— (1R,3S)-3-trifluoromethylcyclohexylamine hydrochloride 1529782-04-4 C7H12F3N*ClH
(1R,3S)-3-trifluoromethylcyclohexylamine hydrochloride
—— 16β-formyloxy-3β-(<i>O</i><sup>4</sup>β-D-glucopyranosyl-<i>O</i><sup>3</sup>-methyl-β-D-fucopyranosyloxy)-14-hydroxy-5β,14β-card-20(22)-enolide 6022-99-7 C37H56O15
16β-formyloxy-3β-(<i>O</i><sup>4</sup>β-D-glucopyranosyl-<i>O</i><sup>3</sup>-methyl-β-D-fucopyranosyloxy)-14-hydroxy-5β,14β-card-20(22)-enolide
—— 6-Dehydro-19-nor-testosteron 6242-39-3 C18H24O2
6-Dehydro-19-nor-testosteron
—— 6'-Hydroxycinchonin 524-63-0 C19H22N2O2
6'-Hydroxycinchonin
—— Caffeoyl-coenzyme A 53034-79-0 C30H42N7O19P3S
Caffeoyl-coenzyme A
—— Zinc ricinoleate 93028-47-8 C36H66O6Zn
Zinc ricinoleate
—— Tiaprost 71116-82-0 C20H28O6S
Tiaprost
—— d-menthyl glyoxalate monohydrate 111969-64-3 C12H22O4
d-menthyl glyoxalate monohydrate
—— [(Z,2S)-5-[[(2R,3R,5S,6S)-2,5-dimethyl-6-[(2E,4E)-3-methyl-5-[(3S,4R,5R,7R,8R)-4,5,8-trihydroxy-5-methyl-1,6-dioxaspiro[2.5]octan-7-yl]penta-2,4-dienyl]oxan-3-yl]amino]-5-oxopent-3-en-2-yl] acetate 146478-73-1 C27H41NO9
[(Z,2S)-5-[[(2R,3R,5S,6S)-2,5-dimethyl-6-[(2E,4E)-3-methyl-5-[(3S,4R,5R,7R,8R)-4,5,8-trihydroxy-5-methyl-1,6-dioxaspiro[2.5]octan-7-yl]penta-2,4-dienyl]oxan-3-yl]amino]-5-oxopent-3-en-2-yl] acetate
—— (S)-tert-butyl 4-bromo-2,3-dihydro-1H-inden-1-ylcarbamate 1307231-21-5 C14H18BrNO2
(S)-tert-butyl 4-bromo-2,3-dihydro-1H-inden-1-ylcarbamate
—— (1S,4S)-2-azabicyclo[2.2.1]hept-5-en-3-one 130931-83-8 C6H7NO
(1S,4S)-2-azabicyclo[2.2.1]hept-5-en-3-one
—— Cinitapride tartrate 1207859-16-2 C25H36N4O10
Cinitapride tartrate
—— (1S)-(+)-2-Azabicyclo[2.2.1]hept-5-en-3-one 130931-83-8 C6H7NO
(1S)-(+)-2-Azabicyclo[2.2.1]hept-5-en-3-one
—— 4-nitro-2,6-bis(pyrrolidin-1'-ylmethyl)phenol 121836-29-1 C16H23N3O3
4-nitro-2,6-bis(pyrrolidin-1'-ylmethyl)phenol
—— 2,3-norbornanediol 14440-78-9 C7H12O2
2,3-norbornanediol
—— (S)-3-amino-4,4,4-trifluorobutanoic acid 151871-99-7 C4H6F3NO2
(S)-3-amino-4,4,4-trifluorobutanoic acid
—— 2,4-Distyrylphenol 2012-21-7 C22H18O
2,4-Distyrylphenol
—— ethyl 2-cyclobutyl-2-oxoacetate 861160-59-0 C8H12O3
ethyl 2-cyclobutyl-2-oxoacetate
—— fluoromethylhexahydropyridine 886216-73-5 C6H12FN
fluoromethylhexahydropyridine
—— 2,6-dibromo-3-nitro-toluene 110127-07-6 C7H5Br2NO2
2,6-dibromo-3-nitro-toluene
—— 3beta-Acetoxy-5alpha-pregn-16-en-20-one 1169-20-6 C23H34O3
3beta-Acetoxy-5alpha-pregn-16-en-20-one
—— 11α-Acetoxy-pregnen-(4)-dion-(3,20) 2268-98-6 C23H32O4
11α-Acetoxy-pregnen-(4)-dion-(3,20)