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-(三氟甲基)-1H-吡唑 | 4-(trifluoromethyl)-1H-pyrazole | 52222-73-8 | C4H3F3N2 |
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4-(N-苄氧羰基)-氨基哌啶 | benzyl piperidin-4-ylcarbamate | 182223-54-7 | C13H18N2O2 |
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4-(N,N-二甲氨基)苯硼酸频那醇酯 | (4-(N,N-dimethylamino)phenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane | 171364-78-6 | C14H22BNO2 |
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4-(N,N-二甲基氨基)萘-1-硼酸频那醇酯 | N,N-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)naphthalen-1-amine | 1007126-41-1 | C18H24BNO2 |
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4-(Boc-氨基)-3,3-二甲基哌啶 | (+/-)-4-t-Butyloxycarbonylamino-3,3-dimethylpiperidine | 544443-41-6 | C12H24N2O2 |
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4-(6-氨基吡啶-3-基)哌嗪-1-羧酸叔丁酯 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate | 571188-59-5 | C14H22N4O2 |
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4-(6-(7-环戊基-6-(二甲基甲酰基)-7H-吡咯并[2,3-D]嘧啶-2-基氨基吡啶-3-基)哌嗪-1-羧酸叔丁酯 | tert-butyl 4-(6-((7-cyclopentyl-6-(dimethylcarbamoyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate | 1374639-78-7 | C28H38N8O3 |
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4-(5-(三氟甲基)-1,2,4-恶二唑-3基)苯甲酸 | 4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzoic acid | 340736-76-7 | C10H5F3N2O3 |
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4-(4-羟基苯基)丁酸 | 4-(4-hydroxyphenyl)butanoic acid | 7021-11-6 | C10H12O3 |
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4-(4-羟基联苯甲基)哌啶-1-氧代丁基-2,2-二甲基苯乙酸甲酯 | methyl 2-(4-(4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoate | 154477-55-1 | C33H39NO4 |
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4-(4-甲氧基苯基)哌嗪-1-甲酰胺 | 4-(4-Methoxyphenyl)piperazine-1-carboxamide | 89026-59-5 | C12H17N3O2 |
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4-(4-溴-3-(1,3-二氧戊环-2-基)苯氧基)苯甲腈 | 4-(4-bromo-3-(1,3-dioxolan-2-yl)phenoxy)benzonitrile | 1217366-74-9 | C16H12BrNO3 |
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4-(4-氯苯基)环己基羧酸 | 4-(4-chlorophenyl)cyclohexane-1-carboxylic acid | 95233-37-7 | C13H15ClO2 |
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4-(4-氯-2-噻吩基)-2-噻唑胺 | 4-(4-chloro-2-thienyl)-2-thiazolamine | 570407-10-2 | C7H5ClN2S2 |
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4-(4-氨基苯基)吗啡啉-3-酮 | 4-(4-aminophenyl)-3-morpholinone | 438056-69-0 | C10H12N2O2 |
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4-(4-氟苯基)-1H-咪唑 | 4-(4-fluorophenyl)-1H-imidazole | 65020-70-4 | C9H7FN2 |
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4-(4-(4,4,5,5-四甲基-1,3,2-二氧杂硼杂环戊烷-2-基)苯氧基)哌啶-1-羧酸叔丁酯 | tert-butyl 4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy]piperidine-1-carboxylate | 889865-34-3 | C22H34BNO5 |
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4-(4,6-二甲氧基三嗪-2-基)-4-甲基吗啉盐酸盐 | 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride | 3945-69-5 | C10H17N4O3*Cl |
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4-(3-氯-4-甲氧基苄基氨基)-5-乙氧羰基-2-甲基亚磺酰嘧啶 | 4-(3-chloro-4-methoxybenzylamino)-5-ethoxycarbonyl-2-methylsulfinylpyrimidine | 330785-82-5 | C16H18ClN3O4S |
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4-(3-氧代-4-吗啉基)硝基苯 | 4-(4-nitrophenyl)-3-morpholinone | 446292-04-2 | C10H10N2O4 |
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4-(3,4-二氯苯基)-1-四氢萘酮 | 4-(3,4-dichlorophenyl)-1-tetralone | 79560-19-3 | C16H12Cl2O |
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4-(3,4-二氯-2-氟苯基氨基)-7-甲氧基喹唑啉-6-醇 | 4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-ol | 1429757-65-2 | C15H10Cl2FN3O2 |
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4-(2’-吡啶基)苯甲酸 | 2-(4-carboxyphenyl)pyridine | 4385-62-0 | C12H9NO2 |
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4-(2-羟基乙基)哌嗪-1-乙烷磺酸钾 | Potassium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate | 82207-62-3 | C8H17KN2O4S |
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4-(2-甲基苯基)苯基硼酸 | p-tolyphenylboronic acid | 491595-36-9 | C13H13BO2 |
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4-(2-氯-9-甲基嘌呤-6-基)吗啉 | 4-(2-chloro-9-methyl-9H-purin-6-yl)morpholine | 1148003-35-3 | C10H12ClN5O |
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4-(2-Boc-氨乙基)哌啶 | tert-butyl 2-(piperidin-4-yl)ethylcarbamate | 165528-81-4 | C12H24N2O2 |
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4-(2-(苄基(叔丁基)氨基)-1-羟基乙基)-2-(羟甲基)苯酚 | α-[(benzyl-tert-butylamino)methyl]-m-xylene-4,α,α'-triol | 24085-03-8 | C20H27NO3 |
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4-(1H-苯并[d]咪唑-2-基)哌啶-1-羧酸叔丁酯 | tert-butyl 4-(1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate | 953071-73-3 | C17H23N3O2 |
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4-(1H-1,2,4-三唑-1-基甲基)苯甲腈 | 4-((1H-1,2,4-triazol-1-yl)methyl)benzonitrile | 112809-25-3 | C10H8N4 |
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4-(1-苯基乙基)间二甲苯 | 1-(1-phenylethyl)-2,4-dimethylbenzene | 6165-52-2 | C16H18 |
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4-(1-氰基环丙基)苯硼酸 | (4-(1-cyanocyclopropyl)phenyl)boronic acid | 1217501-00-2 | C10H10BNO2 |
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4-(1-吡咯烷基磺酰基甲基)苯肼盐酸盐 | 4-((pyrrolidin-1-ylsulfonyl)methyl)phenylhydrazine hydrochloride | 334981-11-2 | C11H17N3O2S*ClH |
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4-(1-(羟基甲基)环丙基)苯硼酸 | 4-(1-(hydroxymethyl)cyclopropyl)phenylboronic acid | 1217501-10-4 | C10H13BO3 |
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4-(1,2,4-三唑-1-基)苯甲醇 | (4-(1H-1,2,4-triazol-1-yl)phenyl)methanol | 143426-50-0 | C9H9N3O |
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4,8-二甲基壬-3,7-二烯-2-醇 | 4,8-dimethylnona-3,7-dien-2-ol | 67845-50-5 | C11H20O |
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4,8-二十二烷基苯并[1,2-B:4,5-B']二噻吩(C12) | 4,8-di(dodecylthio)benzo[1,2-b:4,5-b']dithiophene | 903518-70-7 | C34H54S2 |
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4,7-二羟基香豆素 | 4,7-dihydroxycoumarin | 1983-81-9 | C9H6O4 |
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4,7-二甲基香豆素 | 4,7-dimethyl-coumarin | 14002-90-5 | C11H10O2 |
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4,7-二溴-[1,2,5]噻二唑并[3,4-c]吡啶 | 4,7-dibromo-[1,2,5]thiadiazolo[3,4-c]pyridine | 333432-27-2 | C5HBr2N3S |
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4,7-二氮杂螺[2.5]辛烷-4-甲酸叔丁酯 | tert-butyl 4,7-diazaspiro[2.5]octane-4-carboxylate | 674792-08-6 | C11H20N2O2 |
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4,6-二溴吡啶腈 | 4,6-Dibromopicolinonitrile | 1206247-80-4 | C6H2Br2N2 |
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4,6-二氯靛红 | 4,6-dichloro-1H-indole-2,3-dione | 18711-15-4 | C8H3Cl2NO2 |
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4,6-二氯吲哚-2-甲酸乙酯 | ethyl 4,6-dichloro-1H-indole-2-carboxylate | 53995-82-7 | C11H9Cl2NO2 |
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4,6-二氯-2-(甲基硫代)嘧啶-5-羧酰胺 | 4,6-dichloro-2-(methylsulfanyl)pyrimidine-5-carboxamide | 313339-36-5 | C6H5Cl2N3OS |
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4,6-二氟-1H-吲唑 | 4,6-difluoro-1H-indazole | 885520-26-3 | C7H4F2N2 |
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4,5-二碘咪唑 | 4,5-diiodo-1H-imidazole | 15813-09-9 | C3H2I2N2 |
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4,5-二甲氧基-1-氰基苯并环丁烷 | 3,4-dimethoxy-bicyclo[4.2.0]octa-1,3,5-triene-7-carbonitrile | 35202-54-1 | C11H11NO2 |
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4,5-二溴噻吩-2-甲醛 | 4,5-dibromothiophene-2-carbaldehyde | 38071-22-6 | C5H2Br2OS |
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4,5-二氯-N-辛基-3-异噻唑啉酮 | 10b,11-Dihydro-10b-hydroxy-6H-pyrido<4',3'-4,5>pyrrolo<2,1-a>isoindol-6-on | 64959-81-5 | C14H10N2O2 |
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