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-乙酰氨基环己酮 | N-(4-oxocyclohexyl)acetamide | 27514-08-5 | C8H13NO2 |
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4-乙酰氨基-5-氯-2-乙氧基苯甲酸甲酯 | Methyl 4-acetamido-5-chloro-2-ethoxybenzoate | 4235-43-2 | C12H14ClNO4 |
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4-乙酰氧基苯酚 | hydroquinone monoacetate | 3233-32-7 | C8H8O3 |
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4-乙酰氧基-6,7-二氟-2-乙硫基喹啉-3-羧酸乙酯 | ethyl 4-acetoxy-6,7-difluoro-2-(ethylthio)quinoline-3-carboxylate | 154330-68-4 | C16H15F2NO4S |
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4-乙酰氧基-2-甲基戊烷-2-醇 | 4-acetoxy-2-methylpentan-2-ol | 4833-08-3 | C8H16O3 |
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4-乙酰基萘-1-羧酸 | 4-acetyl-1-naphthoic acid | 131986-05-5 | C13H10O3 |
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4-乙酰基-2-甲基苯甲酸 | 4-acetyl-2-methylbenzoic acid | 55860-35-0 | C10H10O3 |
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4-乙烯基苄基缩水甘油醚 | 2-(4-vinyl-benzyloxymethyl)-oxirane | 113538-80-0 | C12H14O2 |
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4-乙烯基(苯基)乙酸甲酯 | methyl 2-(4-vinylphenyl)acetate | 62667-42-9 | C11H12O2 |
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4-乙基-1-萘甲酸 | 4-ethyl-1-naphthoic acid | 91902-58-8 | C13H12O2 |
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4-三氟甲氧基苯甲酸甲酯 | methyl 4-(trifluoromethoxy)benzoate | 780-31-4 | C9H7F3O3 |
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4-三氟甲基硫代苯硼酸频那醇酯 | 4,4,5,5-tetramethyl-2-(4-((trifluoromethyl)thio)phenyl)-1,3,2-dioxaborolane | 1005206-25-6 | C13H16BF3O2S |
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4-三氟甲基乙酸乙酰苯胺 | 3-oxo-N-(4-(trifluoromethyl)phenyl)butanamide | 351-87-1 | C11H10F3NO2 |
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4-β-羟乙砜基硫酸酯苯胺-2-磺酸 | 2-[(3-sulfo-4-aminobenzene)sulfonyl]ethoxysulfonic acid | 42986-22-1 | C8H11NO9S3 |
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4-{[4-({4-[(E)-2-氰基乙烯基]-2,6-二甲基苯基}氨基)-2-嘧啶基]氨基}苯甲腈盐酸盐(1:1) | Rilpivirine hydrochloride | 700361-47-3 | C22H18N6*ClH |
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4-[[4-(苯基氨基)苯基]亚氨基]环己-2,5-二烯-1-酮 | [1,4]benzoquinone-mono-(4-anilino-phenylimine) | 6201-64-5 | C18H14N2O |
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4-[[2-(4-氯苯基)-4,4-二甲基环己-1-烯基]甲基]哌嗪-1-羧酸叔丁酯 | tert-butyl 4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazine-1-carboxylate | 1228780-71-9 | C24H35ClN2O2 |
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4-[4-(4,4,5,5-四甲基-1,3,2-二氧杂环戊硼烷-2-基)-1H-吡唑-1-基]哌啶-1-甲酸叔丁酯 | tert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate | 877399-74-1 | C19H32BN3O4 |
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4-[3-(三氟甲基)苯基]-1-哌嗪乙醇 | N-2-hydroxyethyl-N'-(3-trifluoromethylphenyl)-piperazine | 40004-29-3 | C13H17F3N2O |
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4-[2-哌啶-1-乙氧基]苯甲酸盐酸盐 | 4-(2-piperidin-1-ylethoxy)benzoic acid hydrochloride | 84449-80-9 | C14H19NO3*ClH |
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4-[2-[(3-乙基-4-甲基-2-氧代-3-吡咯琳)甲酰胺基]乙基]苯磺酰胺 | 4-(2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl)benzenesulfonamide | 119018-29-0 | C16H21N3O4S |
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4-[2-[(1Z)-3-(叔丁氧基)-3-氧代-1-丙烯-1-基]苯基]-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸二乙酯 | diethyl (E)-4-<2-<3-(1,1-dimethylethoxy)-3-oxo-1-propenyl>phenyl>-1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate | 103890-79-5 | C26H33NO6 |
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4-[2-(5-氯-2-甲基苯基)偶氮]-3-羟基-N-(2-甲氧基苯基)-2-萘甲酰胺 | 2-Naphthalenecarboxamide, 4-[(5-chloro-2-methylphenyl)azo]-3-hydroxy-N-(2-methoxyphenyl)- | 21889-28-1 | C25H20ClN3O3 |
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4-[1-(4,5-二氢-4,4-二甲基-2-恶唑基)-1-甲基乙基]苯乙醇对甲苯磺酸酯 | 2-[4-[1-(4,4-dimethyl-5H-oxazol-2-yl)-1-methylethyl]phenyl]ethyl4-methylbenzenesulfonate | 202189-76-2 | C23H29NO4S |
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4-[(三甲基硅基)乙炔基]吗啉 | 1-morpholino-2-trimethylsilyl acetylene | 64024-63-1 | C9H17NOSi |
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4-[(5-溴-4,6-二氯-2-嘧啶)氨基]苯甲腈 | 4-[[(5-bromo-4,6-dichloro)-2-pyrimidinyl]amino]benzonitrile | 269055-75-6 | C11H5BrCl2N4 |
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4-[(5-氯-2-羟基苯基)偶氮]间苯二酚 | 1,3-Benzenediol, 4-((5-chloro-2-hydroxyphenyl)azo)- | 4867-01-0 | C12H9ClN2O3 |
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4-[(2R)-2-(氯甲基)-3-甲基丁基]-1-甲氧基-2-(3-甲氧基丙氧基)苯 | (R)-2-[4-methoxy-3-(3-methoxypropoxyl)]phenylmethyl-3-methyl-1-chlorobutane | 324763-39-5 | C17H27ClO3 |
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4-[(2,3-二氢噻吩并[3,4-b]-1,4-二噁英-2-基)甲氧基]-1-丁烷磺酸钠 | 4-(2,3-dihydrothieno[3,4-b][1,4]dioxin-2-yl-methoxy)-1-butanesulfonic acid sodium salt | 204444-01-9 | C11H15O6S2*Na |
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4-N-Boc-氨基环己酮 | N-(tert-butoxycarbonyl)-4-aminocyclohexanone | 179321-49-4 | C11H19NO3 |
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4-(羟基甲基)-5-甲基-[1,3]二氧代l-2-酮 | 4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one | 91526-18-0 | C5H6O4 |
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4-(甲氨基)安替比林 | 4-methylaminoantipyrine | 519-98-2 | C12H15N3O |
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4-(甲氧基羰基)-3-溴苯甲酸 | 3-bromo-4-methoxycarbonylbenzoic acid | 264272-63-1 | C9H7BrO4 |
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4-(溴甲基)-7-(二乙氨基)香豆素 | 4-(bromomethyl)-7-(diethylamino)-2H-chromen-2-one | 1256259-14-9 | C14H16BrNO2 |
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4-(溴甲基)-2-甲基苯甲酸甲酯 | methyl 4-(bromomethyl)-2-methylbenzoate | 74733-28-1 | C10H11BrO2 |
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4-(溴甲基)-2-氟苯甲酸甲酯 | methyl 4-(bromomethyl)-2-fluoro-benzoate | 85070-57-1 | C9H8BrFO2 |
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4-(氯甲基)苯甲醛 | 4-chloromethylbenzaldehyde | 73291-09-5 | C8H7ClO |
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4-(氯甲基)-5-环丙基-3-(2,6-二氯苯基)-1,2-恶唑 | 4-(chloromethyl)-5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazole | 1268245-50-6 | C13H10Cl3NO |
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4-(氨基磺酰基)苯硼酸 | 4-sulfamoylphenylboronic acid | 613660-87-0 | C6H8BNO4S |
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4-(氨基甲基)吡唑 | (1H-pyrazol-4-yl)methanamine | 37599-59-0 | C4H7N3 |
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4-(氨基甲基)-4-羟基哌啶-1-甲酸叔丁酯 | tert-butyl 4-(aminomethyl)-4-hydroxypiperidine-1-carboxylate | 392331-66-7 | C11H22N2O3 |
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4-(吡唑-1-基)苯甲醛 | 4-(1H-pyrazol-1-yl)benzaldehyde | 99662-34-7 | C10H8N2O |
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4-(叔丁氧基羰基)吡咯烷-2-羧酸-(2S,4s)-甲酯 | methyl (4S)-4-[(tert-butoxycarbonyl)amino]-L-prolinate | 168263-82-9 | C11H20N2O4 |
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4-(叔丁基二甲基锡氧基)-环己醇 | 4-((tert-butyldimethylsilyl)oxy)cyclohexan-1-ol | 126931-29-1 | C12H26O2Si |
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4-(叔丁基二甲基甲硅烷基)氧代-1-丁醇 | 4-(tert-butyldimethylsiloxy)-1-butanol | 87184-99-4 | C10H24O2Si |
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4-(反-4-乙烯基环己基)苯甲腈 | 4-(4-vinylcyclohexyl)benzonitrile | 96184-42-8 | C15H17N |
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4-(二甲基氨基)丁醛 | 4-(dimethylamino)butyraldehyde | 104459-70-3 | C6H13NO |
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4-(二丙基氨基)偶氮苯四氟硼酸盐 | 4-(Dipropylamino)benzenediazonium tetrafluoroborate | 5059-80-3 | C12H18BF4N3 |
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4-(乙酰氨基)-1-苄基-4-苯基哌啶 | N-(1-benzyl-4-phenylpiperidin-4-yl)acetamide | 172733-78-7 | C20H24N2O |
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4-(三氟甲基)苯基三氟甲烷磺酸酯 | p-(trifluoromethyl)phenyl trifluoromethanesulfonate | 146397-87-7 | C8H4F6O3S |
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