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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4,5-二氟-1-茚酮 | 4,5-difluoro-1-indanone | 628732-11-6 | C9H6F2O |
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4,5-二(2-甲氧基乙氧基)-2-硝基苯甲酸甲酯 | methyl 4,5-bis(2-methoxyethoxy)-2-nitrobenzoate | 501684-22-6 | C14H19NO8 |
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4,5,6,7-四氢吡唑并[1,5-a]吡啶-2-羧酸 | 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-2-carboxylic acid | 307313-03-7 | C8H10N2O2 |
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4,5,6,7-四氢-1H-咪唑并[4,5-c]吡啶 | 4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridine | 6882-74-2 | C6H9N3 |
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4,5,6,7-四氢-1-(4-甲氧基苯基)-7-氧代-6-[4-(2-氧代-1-哌啶基)苯基]-1H-吡唑并[3,4-c]吡啶-3-羧酸乙酯 | ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate | 503614-91-3 | C27H28N4O5 |
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4,4’-双[(4-溴苯基)苯氨基]联苯 | N4,N4'-bis(4-bromophenyl)-N4,N4'-diphenyl-[1,1'-biphenyl]-4,4'-diamine | 344782-48-5 | C36H26Br2N2 |
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4,4’-亚甲基双(2-乙基)苯胺 | 4,4’-diamino-3,3’-diethyl diphenyl methane | 19900-65-3 | C17H22N2 |
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4,4’-亚甲基-双-(3-氯-2,6-二乙基苯胺) | 4,4'-methylene-bis-(3-chloro-2,6-diethylaniline) | 106246-33-7 | C21H28Cl2N2 |
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4,4’,4’-三甲氧基苯甲基氯 | 4,4',4''-trimethoxytrityl chloride | 49757-42-8 | C22H21ClO3 |
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4,4-亚乙烯双(N,N-二甲基苯胺) | 1,1-Bis<p-(dimethylamino)phenyl>ethylene | 7478-69-5 | C18H22N2 |
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4,4-二甲基-1,2,3,4-四氢喹啉 | 4,4-dimethyl-1,2,3,4-tetrahydroquinoline | 20364-31-2 | C11H15N |
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4,4-二甲基-1,10-二氮杂三环[6.4.0.02,6]十二碳-2(6),7-二烯-9-酮 | 7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one | 1346674-23-4 | C12H16N2O |
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4,4,4,-三氟丁-2-酮 | 4,4,4-trifluorobutan-2-one | 2366-70-3 | C4H5F3O |
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4,4'-氧代双苯磺酰肼 | diphenylether-4,4'-disulfonyl hydrazide | 80-51-3 | C12H14N4O5S2 |
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4,4'-二羟基-3,3'-联苯二甲酸 | 4,4′-dihydroxy-[1,1′-biphenyl]-3,3′-dicarboxylic acid | 13987-45-6 | C14H10O6 |
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4,4'-二碘-3,3'-二甲基联苯 | 4,4'-diiodo-3,3'-dimethylbiphenyl | 7583-27-9 | C14H12I2 |
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4,4'-二硼酸三苯胺 | triphenylamine-4,4'-bisboronic acid | 862553-94-4 | C18H17B2NO4 |
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4,4'-[1,4-萘二基二-(1E)-2,1-乙烯基]双[N,N-二苯基苯胺] | N,N-diphenyl-4-[2-[4-[2-[4-(N-phenylanilino)phenyl]ethenyl]naphthalen-1-yl]ethenyl]aniline | 952065-58-6 | C50H38N2 |
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4,4'-(重氮胺)二苯磺酸二钠盐 | 4,4'-(Diazoamino)dibenzenesulfonic acid, disodium salt | 56120-28-6 | C12H9N3Na2O6S2 |
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4,4'-(六氟异丙烯)二酞酸酐 | 4,4'-(1,1,1,3,3,3-hexafluoroisopropylidene)diphthalic anhydride | 1107-00-2 | C19H6F6O6 |
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4'-氯-4-溴联苯 | 4-bromo-4'-chloro-1,1'-biphenyl | 23055-77-8 | C12H8BrCl |
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3beta-羟基孕甾-16-烯-20-酮-3-醋酸酯 | 3β-Acetoxy-5α-pregn-16-en-20-on | 1169-20-6 | C23H34O3 |
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3beta,5,14,16beta-四羟基-19-氧代-5beta-心甾-20(22)-烯内酯16-乙酸酯 | 3beta,5,14,16beta-Tetrahydroxy-19-oxo-5betacard-20(22)-enolide 16-acetate | 6980-15-0 | C25H34O8 |
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3.5-二氯-4-羟基苯甲酸甲酯 | methyl 3,5-dichloro-4-hydroxybenzoate | 3337-59-5 | C8H6Cl2O3 |
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3.5-二(4-甲氧羰基苯基)苯硼酸频呢醇酯 | dimethyl 5'-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-[1,1':3',1''-terphenyl]-4,4''-dicarboxylate | 1331745-91-5 | C28H29BO6 |
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3-苄氧基吡啶-5-硼酸频呐醇酯 | 3-(benzyloxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine | 1375302-99-0 | C18H22BNO3 |
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3-苄基-8-(叔丁氧基羰基)-3,8-二氮杂双环[3.2.1]-辛烷 | tert-butyl 3-benzyl-3,8-diazabicyclo[3.2.1]octane-8-carboxylate | 149771-43-7 | C18H26N2O2 |
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3-苄基-6-溴-2-甲氧基喹啉 | 3-benzyl-6-bromo-2-methoxyquinoline | 654655-69-3 | C17H14BrNO |
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3-羰基-1-茚酸 | 3-oxoindan-1-carboxylic acid | 29427-69-8 | C10H8O3 |
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3-羧甲基绕丹宁 | rhodanine 3-acetic acid | 5718-83-2 | C5H5NO3S2 |
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3-羟基苯乙酸 | 3-hydroxyphenylacetic acid | 621-37-4 | C8H8O3 |
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3-羟基异烟酰胺 | 3-hydroxyisonicotinamide | 10128-73-1 | C6H6N2O2 |
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3-羟基头孢 | 3-hydroxy cephalosporin | 54639-48-4 | C28H24N2O5S |
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3-羟基丙酸甲酯 | methyl ester (3-hydroxy) propionic acid | 6149-41-3 | C4H8O3 |
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3-羟基-6,6-二甲基-1-庚烯-4-炔 | 6,6-dimethyl-1-hepten-4-yn-3-ol | 78629-20-6 | C9H14O |
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3-羟基-4-甲氧基苯腈 | 2-methoxy-5-cyanophenol | 52805-46-6 | C8H7NO2 |
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3-羟基-4-甲氧基-2-硝基苯甲酸 | 2-nitro-3-hydroxy-4-methoxybenzoic acid | 71489-74-2 | C8H7NO6 |
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3-羟基-3-甲基氮杂环丁烷-1-甲酸叔丁酯 | tert-butyl 3-hydroxy-3-methylazetidine-1-carboxylate | 1104083-23-9 | C9H17NO3 |
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3-羟基-2-甲氧苯甲醛 | 3-hydroxy-2-methoxybenzaldehyde | 66495-88-3 | C8H8O3 |
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3-羟基-1-金刚烷甲醇 | 3-(hydroxymethyl)adamantan-1-ol | 38584-37-1 | C11H18O2 |
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3-碘联苯 | 3-iodo-1,1'-biphenyl | 20442-79-9 | C12H9I |
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3-碘喹啉 | 3-Iodoquinoline | 79476-07-6 | C9H6IN |
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3-碘吡唑-4-甲酸乙酯 | ethyl 3-iodo-1H-pyrazole-4-carboxylate | 827316-43-8 | C6H7IN2O2 |
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3-碘吡唑-4-甲腈 | 3-iodo-1H-pyrazole-4-carbonitrile | 827316-44-9 | C4H2IN3 |
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3-碘吡唑 | 3-iodo-1H-pyrazole | 4522-35-4 | C3H3IN2 |
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3-碘-6-硝基吲唑 | 3-iodo-6-nitro-1H-indazole | 70315-70-7 | C7H4IN3O2 |
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3-碘-6-氮杂吲哚 | 3-iodo-1H-pyrrolo[2,3-c]pyridine | 956003-24-0 | C7H5IN2 |
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3-硼-4-甲氧基苯甲酸 | 3-borono-4-methoxybenzoic acid | 730971-32-1 | C8H9BO5 |
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3-硼-2-甲氧基苯甲酸 | 3-carboxy-2-methoxy-phenylboronic acid | 913836-10-9 | C8H9BO5 |
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3-硝基-吡咯烷-1-羧酸叔丁酯 | Tert-butyl 3-nitropyrrolidine-1-carboxylate | 1309581-43-8 | C9H16N2O4 |
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