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:
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。
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。
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。
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。
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。
中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
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N-[3-(4-苄基苯氧基)丙基]-N-甲基-beta-丙氨酸 | SC-57461A | 423169-68-0 | C20H25NO3*ClH |
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N-[2-(二乙基氨基)乙基]-2-甲氧基-4-乙酰氨基-5-氯苯甲酰胺 | N-acetylmetoclopramide | 5608-13-9 | C16H24ClN3O3 |
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N-[2-(乙酰基氧基)丙基]-n-[3-[4-(1,1-二甲基丙基)苯基]-2-甲基丙基]-甲酰胺 | 1-(Formyl{2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl}amino)propan-2-yl acetate | 142347-84-0 | C21H33NO3 |
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N-[(S)-(2,3,4,5,6-五氟苯氧基)苯氧基磷酰基]-L-丙氨酸异丙酯 | isopropyl ((S)-(perfluorophenoxy)(phenoxy)phosphoryl)-L-alaninate | 1334513-02-8 | C18H17F5NO5P |
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N-[(R)-[(1,2-二氢-1-甲基磺酰螺[3H-INDOOLE-3,4'-哌啶]-1'-基)羰基]-2-(苯基甲氧基)乙基]-2-[(1,1-二甲基乙氧基)羰基]氨基-2-甲基-丙酰胺 | N-[(R)-[(1,2-Dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperidin]-1'-yl)carbonyl]-2-(phenylmethyloxy)ethyl]-2-[(1,1-dimethyl-ethoxy)carbonyl]amino-2-methyl-propanamide | 159634-87-4 | C32H44N4O7S |
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N-[(9H-芴-9-甲氧基)羰基]-L-苏氨酸苯基甲酯 | N-(fluoren-9-ylmethoxycarbonyl)-L-threonine benzyl ester | 73724-48-8 | C26H25NO5 |
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N-[(9H-芴-9-基甲氧基)羰基]-3-[(苯基甲基)硫代]-D-缬氨酸 | Fmoc-S-benzyl-D-penicillamine | 139551-73-8 | C27H27NO4S |
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N-[(4-硝基苯基)-甲基磺酰基]吡咯烷 | 1-(4-nitrophenylmethylsulfonyl)pyrrolidine | 340041-91-0 | C11H14N2O4S |
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N-[(3aS,4R,6S,6aR)-四氢-6-羟基-2,2-二甲基-4H-环戊烯并-1,3-二氧戊环-4-基]氨基甲酸苄酯 | benzyl ((3aS,4R,6S,6aR)-6-hydroxy-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)carbamate | 274693-53-7 | C16H21NO5 |
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N-[(2S)-4-甲基-1-[(2R)-2-甲基环氧乙烷-2-基]-1-氧代-2-戊基]氨基甲酸叔丁酯 | tert-butyl ((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)carbamate | 247068-82-2 | C14H25NO4 |
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N-[(2R,3S)-2-(2,5-二氟苯基)四氢-5-氧代-2H-吡喃-3-基]氨基甲酸叔丁酯 | tert-butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl)carbamate | 951127-25-6 | C16H19F2NO4 |
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N-[(1r,2s)-1-[[(环丙基磺酰基)氨基]羰基]-2-乙烯环丙基]氨基甲酸1,1-二甲基乙酯 | tert-butyl ((1R,2S)-1-{[(cyclopropylsulfonyl)amino]carbonyl}-2-vinylcyclopropyl)carbamate | 630421-48-6 | C14H22N2O5S |
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N-FMOC-L-金刚烷甘氨酸 | (2S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-2-(adamantan-1-yl)acetic acid | 1221793-29-8 | C27H29NO4 |
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N-Cbz-4-氧代-3-吡咯烷甲酸乙酯 | 1-benzyl 3-ethyl 4-oxopyrrolidine-1,3-dicarboxylate | 51814-19-8 | C15H17NO5 |
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N-CBZ-S-2-氮杂环丁烷-1-羧酸 | (2S)-1-(benzyloxycarbonyl)azetidine-2-carboxylic acid | 25654-52-8 | C12H13NO4 |
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N-Boc-内-3-氨基托烷 | tert-butyl (1S,5S)-3-amino-8-azabicyclo[3.2.1]octane-8-carboxylate | 207405-68-3 | C12H22N2O2 |
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N-Boc-5-溴邻氨基苯甲酸 | 5-bromo-2-((tert-butoxycarbonyl)amino)benzoic acid | 306937-20-2 | C12H14BrNO4 |
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N-Boc-5,7-二氯-1,2,3,4-四氢异喹啉-6-羧酸 | 2-(tert-butoxycarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid | 851784-82-2 | C15H17Cl2NO4 |
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N-Boc-4-哌啶酮-3-甲酸甲酯 | methyl 1-tert-butoxycarbonyl-4-oxo-3-piperidinecarboxylate | 161491-24-3 | C12H19NO5 |
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N-Boc-4-哌啶甲醇 | tert-butyl 4-(hydroxymethyl)piperidin-1-carboxylate | 123855-51-6 | C11H21NO3 |
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N-Boc-3-吡咯啉 | N-(tert-butoxycarbonyl)-3-pyrroline | 73286-70-1 | C9H15NO2 |
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N-Boc-2-氯乙胺 | tert-butyl N-(2-chloroethyl)carbamate | 71999-74-1 | C7H14ClNO2 |
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N-BOC-反式-3,4-二羟基-四氢吡咯 | trans tert-butyl 3,4-dihydroxypyrrolidine-1-carboxylate | 298681-10-4 | C9H17NO4 |
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N-BOC-4-甲氧基吲哚 | tert-butyl 4-methoxy-1H-indole-1-carboxylate | 1093759-59-1 | C14H17NO3 |
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N-2,3-二氢-1H-茚-2-基-n-甲基胺盐酸盐 | 2-(methylamino)indan | 24445-44-1 | C10H13N |
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N-(苯氧基乙酰基)-2'-脱氧腺苷 | N<sup>6</sup>-(phenoxyacetyl)-2'-deoxyadenosine | 110522-74-2 | C18H19N5O5 |
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N-(氯乙酰)- 4-(三氟甲氧基) 苯胺 | 2-chloro-N-(4-(trifluoromethoxy)phenyl)acetamide | 161290-85-3 | C9H7ClF3NO2 |
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N-(异丙氧羰基)-L-缬氨酸 | N-isopropoxycarbonyl-L-valine | 140923-27-9 | C9H17NO4 |
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N-(p-羟基苯乙基)-n-(2-溴-5-羟基-4-甲氧基苄基)甲酰胺 | N-(4-hydroxyphenethyl)-N-(2-bromo-5-hydroxy-4-methoxybenzyl)formamide | 122584-18-3 | C17H18BrNO4 |
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N-(9-((2R,3R,4R,5R)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-3-氟-4-羟基四氢呋喃-2-基)-9H-嘌呤-6-基)苯甲酰胺 | N-(9-((2R,3R,4R,5R)-5-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-3-fluoro-4-hydroxytetrahydrofuran-2-yl)-9H-purin-6-yl)benzamide | 136834-21-4 | C38H34FN5O6 |
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N-(6-甲酰基-4-氧代-1H-蝶啶-2-基)乙酰胺 | N<sup>2</sup>-acetyl-6-formylpterin | 29769-49-1 | C9H7N5O3 |
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N-(6-氯-5-甲基吡啶-2-基)-1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙烷-1-羧酰胺 | N-(6-chloro-5-methylpyridin-2-yl)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamide | 936727-68-3 | C17H13ClF2N2O3 |
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N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-氨基嘧啶 | 6-methyl-1-N-(4-(pyridin-3-yl)pyrimidin-2-yl)benzene-1,3-diamine | 152460-10-1 | C16H15N5 |
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N-(5-(4,5-二氢-(1H)-吲哚-2-基)-2-羟基-5,6,7,8-四氢萘-1-基)甲烷磺酰胺氢溴酸 | A 61603 | 107756-30-9 | BrH*C14H19N3O3S |
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N-(5,5,8,8-四甲基-5,6,7,8-四氢-2-萘)乙酰胺 (他米巴罗汀) | N-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acetamide | 139162-43-9 | C16H23NO |
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N-(4-羟基戊烷酰基)-N-{[2'-(2H-四唑-5-基)-4-联苯基]甲基}-L-缬氨酸 | 4-Hydroxyvalsartan | 188259-69-0 | C24H29N5O4 |
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N-(4-甲氧基苄基)-n-甲氧基甲基-n-三甲基甲硅烷基甲胺 | 4-methoxy-N-(methoxymethyl)-N-[(trimethylsilyl)methyl]-benzenemethanamine | 433289-59-9 | C14H25NO2Si |
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N-(4-烯丁基)邻苯二甲酰亚胺 | 1-phthalimido-3-butene | 52898-32-5 | C12H11NO2 |
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N-(4-溴-2-甲基苯基)氨基甲酸叔丁酯 | (4-bromo-2-methylphenyl)carbamic acid tert-butyl ester | 306937-14-4 | C12H16BrNO2 |
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N-(4-氯苯甲酰基)-酪胺 | 4-chloro-N-(4-hydroxyphenethyl)benzamide | 41859-57-8 | C15H14ClNO2 |
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N-(4-氯苯基)-N'-[4-氯-3-(三氟甲基)苯基]脲 | cloflucarban | 369-77-7 | C14H9Cl2F3N2O |
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N-(4-氨基苯基)-5-氯-2-羟基苯甲酰胺 | N-(4-aminophenyl)-5-chloro-2-hydroxybenzamide | 63565-17-3 | C13H11ClN2O2 |
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N-(4-氨基-5-甲氧基-2-甲基苯基)苯甲酰胺 | 2-methoxy-4-benzoylamino-5-methyl-aniline | 99-21-8 | C15H16N2O2 |
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N-(4-氟苯基)-n-(4-羟基苯基)环丙烷-1,1-二羧酰胺 | N-(4-fluorophenyl)-N-(4-hydroxyphenyl)cyclopropane-1,1-dicarboxamide | 849217-60-3 | C17H15FN2O3 |
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N-(4-氟-2-甲氧基-5-硝基苯基)-4-(1-甲基-1H-吲哚-3-基)-2-嘧啶胺 | N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine | 1421372-94-2 | C20H16FN5O3 |
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N-(4-乙烯基苄基)-N,N-二甲胺 | N-(4-vinylbenzyl)-N,N-dimethylamine | 2245-52-5 | C11H15N |
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N-(4''-溴[1,1'4',1''-三联苯-4-基)-N-苯基-1-萘胺 | N-(4"-bromo-[1,1':4',1"-terphenyl]-4-yl)-N-phenylnaphthalen-1-amine | 912637-92-4 | C34H24BrN |
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N-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺 | N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine | 162012-67-1 | C14H7ClF2N4O2 |
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N-(3-氯-4-氟苯基)-6-硝基-7-[[(3S)-四氢-3-呋喃基]氧基]-4-喹唑啉胺 | 4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline | 314771-88-5 | C18H14ClFN4O4 |
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N-(3-乙酰基苯基)-n-甲基乙酰胺 | N-(3-acetylphenyl)-N-methylacetamide | 325715-13-7 | C11H13NO2 |
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