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-(3-氨基-4-氯苯甲酰)苯甲酸 | NSC 74496 | 118-04-7 | C14H10ClNO3 |
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2-(3-氟苯基)-1-[4-(甲硫基)苯基]乙酮 | 2-(3-fluorophenyl)-1-(4-methylsulfanylphenyl)ethanone | 301699-27-4 | C15H13FOS |
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2-(3-哌啶基)乙醇盐酸盐 | 2-(piperidin-3-yl)ethanol hydrochloride | 16780-04-4 | C7H15NO*ClH |
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2-(3,4-二甲基苯基)-1,2-二氢-5-甲基-3H-吡唑-3-酮 | 2-(3,4-dimethylphenyl)-1,2-dihydro-5-methyl-3H-pyrazol-3-one | 277299-70-4 | C12H14N2O |
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2-(2-羟基苯基)-4H-苯并[e][1,3]恶嗪-4-酮 | 2-(2-hydroxyphenyl)-4H-benzo[e][1,3]oxazin-4-one | 1218-69-5 | C14H9NO3 |
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2-(2-羟基乙氧基)乙基十六烷酸酯 | 2-(2-hydroxyethoxy)ethyl palmitate | 36381-62-1 | C20H40O4 |
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2-(2-甲氧羰基苯基)乙酸 | 2-(2-(methoxycarbonyl)phenyl)acetic acid | 14736-49-3 | C10H10O4 |
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2-(2-氯苯甲酰基)吡啶 | 2-(2-Chlorbenzoyl)-pyridin | 1694-57-1 | C12H8ClNO |
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2-(2-氯乙氧基)乙酸 | 2-(2-chloroethoxy)acetic acid | 14869-41-1 | C4H7ClO3 |
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2-(2-氯乙氧基)-5-硝基苯甲醛 | 2-(2-chloroethoxy)-5-nitrobenzaldehyde | 110837-53-1 | C9H8ClNO4 |
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2-(2-氯-1-亚乙基)酰肼甲酸甲酯 | amidrazone | 155742-64-6 | C4H8ClN3O2 |
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2-(2-氨基-5-溴-苯甲酰基)吡啶 | 2-amino-5-bromobenzoyl pyridine | 1563-56-0 | C12H9BrN2O |
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2-(2-氧代-1-吡咯烷基)乙基甲基丙烯酸酯 | N-(2-methacryloyloxyethyl)pyrrolidone | 946-25-8 | C10H15NO3 |
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2-(2-氟-4-羟基苯基)乙酸甲酯 | methyl 2-(2-fluoro-4-hydroxyphenyl)acetate | 91361-59-0 | C9H9FO3 |
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2-(2-乙氧基苯氧基)溴乙烷 | 2-(2-ethoxyphenoxy)ethyl bromide | 3259-03-8 | C10H13BrO2 |
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2-(2-乙基己基)噻吩 | 2-(2-ethylhexyl)thiophen | 4891-44-5 | C12H20S |
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2-(2-乙基-1-哌啶基)乙胺 | 2-(2-Ethyl-piperidin-1-yl)-ethylamine | 22014-04-6 | C9H20N2 |
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2-(2-丙炔-1-基)丙二酸二乙酯 | diethyl propargylmalonate | 17920-23-9 | C10H14O4 |
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2-(2-(苄氧基)乙基)丙二酸二乙酯 | diethyl (2-(benzyloxy)ethyl)malonate | 41478-45-9 | C16H22O5 |
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2-(2-(3-(2-(7-氯-2-喹啉基)-乙烯基苯基)-3-羟基丙基)苯基)-2-丙醇 | (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methylethyl)phenyl]-propan-1-ol | 142569-70-8 | C29H28ClNO2 |
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2-(2,6-二氧代-哌啶-3-基)-4-氟基-异吲哚-1,3-二酮 | 2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione | 835616-60-9 | C13H9FN2O4 |
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2-(2,4-二氯苯基)-4-(二氟甲基)-2,4-二氢-5-甲基-3H-1,2,4-三唑-3-酮 | 1-(2,4-dichlorophenyl)-3-methyl-4-difluoromethyl-1,2,4-triazol-5-one | 111992-16-6 | C10H7Cl2F2N3O |
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2-(2',4'-二甲苯氨基)-3-甲基-6-二乙氨基荧烷(B15) | Spiro[isobenzofuran-1(3H),9'-[9H]xanthen]-3-one, 6'-(diethylamino)-2'-[(2,4-dimethylphenyl)amino]-3'-methyl- | 36431-22-8 | C33H32N2O3 |
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2-(1H-吲唑-6-基硫代)-N-甲基苯甲酰胺 | 2-((1H-indazol-6-yl)thio)-N-methylbenzamide | 944835-85-2 | C15H13N3OS |
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2-(1-金刚烷基)乙酸甲酯 | methyl (1-adamantyl)acetate | 27174-71-6 | C13H20O2 |
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2-(1-金刚烷基)-4-溴苯酚 | 2-(1-adamantyl)-4-bromophenol | 104224-68-2 | C16H19BrO |
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2-(1-金刚烷基)-4-溴苯甲醚 | 2-(1-adamantyl)-4-bromoanisole | 104224-63-7 | C17H21BrO |
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2-(1-甲基-2-亚吡咯烷基)乙酸甲酯 | Acetic acid, (1-methyl-2-pyrrolidinylidene)-, methyl ester | 78167-68-7 | C8H13NO2 |
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2-(1-(乙基磺酰基)-3-(4-(7-((2-(三甲基甲硅烷基)乙氧基)甲基)-7H-吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑-1-基)氮杂环丁烷-3-基)乙腈 | 2-(1-(ethylsulfonyl)-3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl) azetidin-3-yl) acetonitrile | 1187594-13-3 | C22H31N7O3SSi |
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2-((叔丁氧羰基)氨基)-2-甲基丙酸甲酯 | methyl 2-(tert-butoxycarbonylamino)-2-methylpropanoate | 84758-55-4 | C10H19NO4 |
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2-((丁酰基)氨基)丙酸 | butyrylalnine | 59875-04-6 | C7H13NO3 |
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2-((4-氟苄基)-氨基)-乙醇 | 2-(4-fluoro-benzyl-amino)-ethanol | 22116-33-2 | C9H12FNO |
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2-((2R,4aS,6S,7R,8S,8aS)-7,8-二((叔丁基二甲基硅)氧基)-6-((S,E)-1-((叔丁基二甲基硅)氧基)-3-(三甲基硅基)烯丙基)八氢吡喃[3,2-b]吡喃-2-基)乙酸甲酯 | Methyl 2-((2R,4aS,6S,7R,8S,8aS)-7,8-bis((tert-butyldimethylsilyl)oxy)-6-((S,E)-1-((tert-butyldimethylsilyl)oxy)-3-(trimethylsilyl)allyl)octahydropyrano[3,2-b]pyran-2-yl)acetate | 185411-11-4 | C35H72O7Si4 |
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2-((2,6-二氯苯基)甲氧基)乙醇 | 2-(2,6-dichlorobenzyloxy)ethanol | 85309-91-7 | C9H10Cl2O2 |
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2-((2,6-二氟苄基)(乙氧羰基)氨基)-4-甲基-5-(4-硝基苯基)噻吩-3-羧酸乙酯 | ethyl 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-methyl-5-(4-nitrophenyl)thiophene-3-carboxylate | 308831-94-9 | C24H22F2N2O6S |
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2-((1R,5R)-3-苯基-7-氧-4-硫代-2,6-二氮杂双环[3.2.0]庚烯基)-3-甲基丁烯醇亚硝基苯 | 2-((1<i>R</i>)-3-benzyl-7-oxo-(1<i>r</i><i>H</i>,5<i>c</i><i>H</i>)-4-thia-2,6-diaza-bicyclo[3.2.0]hept-2-en-6-yl)-3-methyl-but-2-enoic acid 4-nitro-benzyl ester | 192049-49-3 | C23H21N3O5S |
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2-((1H-1,2,4-三唑-5-基)硫基)-N-(4-(金刚烷-1-基)苯基)乙酰胺 | MGH-CP1 | 896657-58-2 | C20H24N4OS |
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2,9-二苯基-1,10-菲咯啉 | 2,9-diphenyl-1,10-phenanthroline | 25677-69-4 | C24H16N2 |
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2,9-二氮杂螺[5.5]十一烷-2-羧酸叔丁酯 | tert-butyl 2,9-diazaspiro[5.5]undecane-2-carboxylate | 189333-03-7 | C14H26N2O2 |
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2,8-二氮杂螺[4.5]癸烷-2-羧酸叔丁酯盐酸盐 | tert-butyl 2,8-diazaspiro[4.5]decane-2-carboxylate hydrochloride | 869976-20-5 | C13H24N2O2*ClH |
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2,7-二羟基-9-芴酮 | 2,7-dihydroxy-9H-fluoren-9-one | 42523-29-5 | C13H8O3 |
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2,7-二甲氧基-1,4,5,8-四氢萘 | 2,7-Dimethoxy-1,4,5,8-tetrahydro-naphthalin | 1614-82-0 | C12H16O2 |
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2,7-二溴-9,9-二氟芴 | 2,7-dibromo-9,9-difluoro-9H-fluorene | 1229603-71-7 | C13H6Br2F2 |
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2,7-二氯芴 | 2,7-dichloro-9H-fluorene | 7012-16-0 | C13H8Cl2 |
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2,6-双[(3aR,8aS)-(+)-8H-茚[1,2-d]恶唑啉-2-基]吡啶 | 2,6-bis[(3aR,8aS)-3a,8a-dihydro-8H-indeno[1,2-d]oxazolin-2-yl]pyridine | 357209-32-6 | C25H19N3O2 |
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2,6-双(二叔丁基膦基甲基)吡啶 | 2,6-bis((di-tertbutylphosphino)methyl)pyridine | 338800-13-8 | C23H43NP2 |
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2,6-二甲基四氢-4H-吡喃-4-酮 | 2,6-dimethyl-tetrahydro-pyran-4-one | 1073-79-6 | C7H12O2 |
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2,6-二甲基-4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)苯胺 | 2,6-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline | 1004761-68-5 | C14H22BNO2 |
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2,6-二溴-4-苯基-苯酚 | 3,5-dibromo-4-hydroxybiphenyl | 4400-05-9 | C12H8Br2O |
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2,6-二溴-4-甲基苯胺 | 2,6-Dibromo-4-methylaniline | 6968-24-7 | C7H7Br2N |
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