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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2-[(4-氯苯基)(4-哌啶氧基)甲基]吡啶对硝基苯甲酸盐 | 2-((4-Chlorophenyl)(piperidin-4-yloxy)methyl)pyridine 4-nitrobenzoate | 161558-45-8 | C24H24ClN3O5 |
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2-[(4-氯苯基)(4-哌啶基氧基)甲基]吡啶 | 2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine | 122368-54-1 | C17H19ClN2O |
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2-[(3-溴苯甲酰基)氨基]-4-氯苯甲酸 | 2-[(3-Bromobenzoyl)amino]-4-chlorobenzoic acid | 827325-60-0 | C14H9BrClNO3 |
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2-[(1H-吡咯并[2,3-b]吡啶-5-基)氧基]-4-[4-[[2-(4-氯苯基)-4,4-二甲基环己-1-烯基]甲基]哌嗪-1-基]苯甲酸甲酯 | methyl 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoate | 1235865-76-5 | C34H37ClN4O3 |
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2-[(1H-吡咯并[2,3-B]吡啶-5-基)氧基]-4-[4-[[2-(4-氯苯基)-4,4-二甲基环己-1-烯基]甲基]哌嗪-1-基]苯甲酸 | 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid | 1235865-77-6 | C33H35ClN4O3 |
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2-[(1,1-二甲基乙基)(苯基甲基)氨基]-1-[4-羟基-3-(羟基-甲基)苯基]乙酮沙丁胺醇 | N-benzylsalbutamone | 64092-10-0 | C20H25NO3 |
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2-F-RC(N-BZ)亚磷酰胺单体 | N<sup>4</sup>-benzoyl-2'-deoxy-2'-fluoro-5'-O-(4,4'-dimethoxytrityl)cytidine 3'-(β-cyanoethyl N,N-diisopropylphosphoramidite) | 161442-19-9 | C46H51FN5O8P |
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2-Boc-氨基苯甲醛 | tert-butyl (2-formylphenyl)carbamate | 74965-38-1 | C12H15NO3 |
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2-Boc-8-氧代-2-氮杂螺[4.5]癸烷 | tert-butyl 8-oxo-2-azaspiro[4.5]decane-2-carboxylate | 1272758-17-4 | C14H23NO3 |
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2-Boc-6-氧代-2-氮杂螺[3.3]庚烷 | tert-butyl 6-oxo-2-azaspiro[3.3]heptane-2-carboxylate | 1181816-12-5 | C11H17NO3 |
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2-BOC-2,8-二氮杂-螺[4.5]癸烷 | tert-butyl 2,8-diazaspiro[4.5]decane-2-carboxylate | 336191-17-4 | C13H24N2O2 |
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2-BIS(4-羟苯基)甲基苄醇 | phenolphthalol | 81-92-5 | C20H18O3 |
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2-(羟基苯基甲基)-丙烯酸甲酯 | methyl 3-hydroxy-2-methylidene-3-phenylpropionate | 18020-59-2 | C11H12O3 |
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2-(羟亚氨基)乙酰乙酸乙酯 | ethyl 2-hydroxyimino-3-oxobutanoate | 5408-04-8 | C6H9NO4 |
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2-(糠基硫基)乙酰胺 | 2-furfurylthioacetamide | 86251-28-7 | C7H9NO2S |
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2-(甲硫基)-4-氯-5-溴-6-甲基嘧啶 | 5-bromo-4-chloro-6-methyl-2-(methylthio)pyrimidine | 17119-74-3 | C6H6BrClN2S |
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2-(甲基磺酰)苯酚 | 2-hydroxyphenyl methyl sulfone | 27489-33-4 | C7H8O3S |
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2-(甲基硫代)甲基丙烯酸乙酯 | 2-(methylthio)ethyl methacrylate | 14216-23-0 | C7H12O2S |
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2-(溴甲基)苯乙酸甲酯 | methyl 2-[2-(bromomethyl)phenyl]acetate | 13737-37-6 | C10H11BrO2 |
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2-(氨甲基)吗啉 | 1-morpholin-2-ylmethanamine | 116143-27-2 | C5H12N2O |
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2-(异丙基磺酰基)苯胺 | 2-(isopropylsulfonyl)aniline | 76697-50-2 | C9H13NO2S |
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2-(二苯基甲基)奎宁环-3-酮 | 2-benzhydryl-3-quinuclidinone | 32531-66-1 | C20H21NO |
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2-(二甲基氨基)-2-氧代乙基 2-(4-羟基苯基)乙酸酯 | 2-(dimethylamino)-2-oxoethyl 2-(4-hydroxyphenyl)acetate | 59721-16-3 | C12H15NO4 |
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2-(乙酰氨基)-3-硝基苯甲酸甲酯 | 2-acetylamino-3-nitro-benzoic acid methyl ester | 95067-27-9 | C10H10N2O5 |
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2-(乙酰氨基)-2-脱氧-beta-D-吡喃半乳糖基胺3,4,6-三乙酸酯 | 1-amino 2-acetamido 1,2-dideoxy 3,4,6-tri-O-acetyl-β-D-galactopyranose | 39541-22-5 | C14H22N2O8 |
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2-(乙氧羰基)乙烯基乙酸二甲基丁二醇酯 | ethyl (2E)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)acrylate | 1009307-13-4 | C11H19BO4 |
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2-(N,N-DiBOC-氨基)-5-溴吡啶 | tert-butyl N-(5-bromo-2-pyridyl)-N-tert-butoxycarbonyl-carbamate | 209959-28-4 | C15H21BrN2O4 |
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2-(Boc-氨基)异烟酸甲酯 | methyl 2-((tert-butoxycarbonyl)amino)isonicotinate | 639091-75-1 | C12H16N2O4 |
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2-(Boc-氨基)-6-羟基螺[3.3]庚烷 | tert-butyl (6-hydroxyspiro[3.3]heptan-2-yl)carbamate | 1000933-99-2 | C12H21NO3 |
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2-(8-氟-3-(2-甲氧基-5-(三氟甲基)苯基)-2-氧代-1,2,3,4-四氢喹唑啉-4-基 | {8-fluoro-3-[2-methoxy-5-(trifluoromethyl)phenyl]-2-oxo-1,2,3,4-tetrahydroquinazoline-4-yl}methyl acetate | 917389-21-0 | C19H16F4N2O4 |
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2-(5-苯基-1H-吲哚-3-基)乙酸 | 5-phenyl-indole-3-acetic acid | 168649-23-8 | C16H13NO2 |
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2-(5-溴-2-氟苄基)苯并噻吩 | 2-(5-bromo-2-fluorobenzyl)benzo[b]thiophene | 1034305-17-3 | C15H10BrFS |
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2-(5-氨基-1,2,4-噻二唑-3-基)-2(Z)-甲氧基亚胺基乙酸 S-巯基苯并噻唑酯 | (Z)-(5-amino-[1,2,4]thiadiazol-3-yl)methoxyiminothioacetic acid S-benzothiazol-2-yl ester | 89604-91-1 | C12H9N5O2S3 |
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2-(5,5-二甲基-2-氧代-1,3,2-二氧磷杂环己烷-2-基)-1-羟基-2-甲基-3,4-二氢-2H-1lambda5-吡咯-1-基 | 2-methyl-2-(5,5-dimethyl-2-oxo-1,3,2-dioxaphosphinan-2-yl)-3,4-dihydro-2H-pyrrole 1-oxide | 934182-09-9 | C10H18NO4P |
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2-(4-硝基苯基)吡啶 | 2-(4-nitrophenyl)pyridine | 4282-47-7 | C11H8N2O2 |
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2-(4-硝基苯基)丁酸 | 2RS-(4-nitrophenyl)butanoic acid | 7463-53-8 | C10H11NO4 |
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2-(4-甲磺酰基苯基)-1-(6-甲基吡啶-3-基)-乙酮 | 1-(6-methyl-3-pyridinyl)-2-[4-(methylsulfonyl)phenyl]ethanone | 221615-75-4 | C15H15NO3S |
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2-(4-甲氧基-3-甲基苯基)-4,4,5,5-T乙基-1,3,2-二氧杂硼杂环戊烷 | 2-(4-methoxy-3-methylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane | 214360-63-1 | C14H21BO3 |
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2-(4-溴苯基)乙酸叔丁酯 | tert-butyl 2-(4-bromophenyl)acetate | 33155-58-7 | C12H15BrO2 |
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2-(4-溴苯基)-丙二酸-1,3-二乙酯 | 2-(4-bromophenyl)-malonic acid dimethyl ester | 149506-35-4 | C11H11BrO4 |
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2-(4-溴苯基)-2-羟基丙酸 | 2-(4-bromophenyl)-2-hydroxypropanoic acid | 58244-32-9 | C9H9BrO3 |
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2-(4-溴-3-氧代丁基)-1H-异吲哚-1,3(2H)-二酮 | 2-(4-bromo-3-oxobutyl)isoindoline-1,3-dione | 51132-00-4 | C12H10BrNO3 |
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2-(4-溴-2-氟苯氧基)丙烷 | 4-bromo-2-fluoro-1-isopropoxybenzene | 202865-80-3 | C9H10BrFO |
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2-(4-氯苯基)-4,4-二甲基-1-环己烯-1-羧醛 | 2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enecarbaldehyde | 1228837-05-5 | C15H17ClO |
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2-(4-氟苯基)-5-[(5-碘-2-甲基苯基)甲基]噻吩 | 2-(4-fluorophenyl)-5-(5-iodo-2-methylbenzyl)thiophene | 898566-17-1 | C18H14FIS |
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2-(4-异丙基噻唑-2-基)-7-甲氧基-8-甲基喹啉-4-醇 | 2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-ol | 923289-21-8 | C17H18N2O2S |
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2-(4-吗啉基)-16-(1-吡咯基)-雄甾-3,17-二醇 | (2β,3α,5α,16β,17β)-2-(4-morpholinyl)-16-(1-pyrrolidinyl)androstane-3,17-diol | 119302-20-4 | C27H46N2O3 |
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2-(4-(2-羟基乙基)苯基)-2-甲基丙酸 | 2-(4-(2-hydroxyethyl)phenyl)-2-methylpropionic acid | 552301-45-8 | C12H16O3 |
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2-(3-醛基-4-羟基苯基)-4-甲基噻唑-5-羧酸乙酯 | ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate | 161798-01-2 | C14H13NO4S |
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2-(3-溴-6-甲基-2-吡嗪酮-1(2H)-基)乙酸乙酯 | 3-bromo-1-(ethoxycarbonylmethyl)-6-methylpyrazinone | 221136-66-9 | C9H11BrN2O3 |
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