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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1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸-(1'-rac-甘油)(钠盐) | 1-Palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol, sodium salt | 268550-95-4 | C40H76NaO10P |
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1-异吲哚酮-5-硼酸频哪醇酯 | 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isoindolin-1-one | 376584-62-2 | C14H18BNO3 |
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1-己基邻碳硼烷 | 1,2-Dicarbadodecaborane(12), 1-hexyl- | 20740-05-0 | C8H14B10 |
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1-叔丁基哌啶-4-酮 | 1-tert-butyl-piperidin-4-one | 1465-76-5 | C9H17NO |
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1-去羧基酮咯酸 | 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2a]pyrrole | 113502-55-9 | C14H13NO |
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1-二氟甲基-4-氨基吡唑盐酸盐 | 1-(difluoromethyl)-1H-pyrazol-4-amine hydrochloride | 1221726-31-3 | C4H6ClF2N3 |
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1-乙酰基-N,N-二乙基-麦角酰胺 | 1-acetyl-6-methyl-9,10-didehydro-ergoline-8β-carboxylic acid diethylamide | 3270-02-8 | C22H27N3O2 |
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1-乙酰基-6-氯-1H- 吲哚-3-乙酯 | 6-chloro-3-acetoxy-1-acetylindole | 108761-33-7 | C12H10ClNO3 |
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1-乙酰基-4-(4-羟基苯基)哌嗪 | N-acetyl-N'-(4-hydroxyphenyl)piperazine | 67914-60-7 | C12H16N2O2 |
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1-乙酰基-1H-吲唑(7ci,8ci,9ci) | 1-acetylindazole | 13436-49-2 | C9H8N2O |
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1-乙氧羰基-4-(4-羟基苯基)哌嗪 | 4-(4-hydroxy-phenyl)-piperazine-1-carboxylic acid ethyl ester | 67914-99-2 | C13H18N2O3 |
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1-乙氧甲酰咪唑 | ethyl 1-imidazolecarboxylate | 19213-72-0 | C6H8N2O2 |
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1-乙基-3-甲基-1H-咪唑-3-鎓二丁基磷酸酯 | 1-ethyl-3-methylimidazolium dibutyl phosphate | 869858-84-4 | C6H11N2*C8H18O4P |
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1-丙酮,2-羟基-1-(4-甲氧苯基)-2-甲基- | 2-hydroxy-1-(4-methoxyphenyl)-2-methyl-1-propanone | 15482-17-4 | C11H14O3 |
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1-丙炔-1-基膦酸 | 1,2-propadienylphosphonic acid | 34163-96-7 | C3H5O3P |
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1-三甲基苯磺酰基-1,2,4-三唑 | 1-(mesitylen-2-sulfonyl)-1H-1,2,4-triazole | 54230-59-0 | C11H13N3O2S |
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1-[[2-(4-氯苯基)乙基]氨基]-2-氯丙烷盐酸盐 | 2-chloro-N-(4-chlorophenethyl)propan-1-amine hydrochloride | 953789-37-2 | C11H15Cl2N*ClH |
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1-[[2-(4-氯苯基)-4,4-二甲基-1-环己烯-1-基]甲基]哌嗪二盐酸盐 | 1-((4'-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazine dihydrochloride | 1628047-87-9 | C19H29Cl3N2 |
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1-[[(6R,7R)-7-氨基-2-羧基-8-氧代-5-硫杂-1-氮杂二环[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-B]哒嗪碘化物 | 7-amino-3-[(imidazo[1,2-b]pyridazinium-1-yl)methyl]-3-cephem-4-carboxylate hydroiodide | 197897-11-3 | C14H13N5O3S*HI |
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1-[4-(4-氯苯基)-2-羟基-正丁基]咪唑 | 1-(2-hydroxy-4-(4-chlorophenyl)butyl)-1H-imidazole | 67085-11-4 | C13H15ClN2O |
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1-[2-氟-6-(三氟甲基)苄基]-6-甲基嘧啶-2,4(1H,3H)-二酮 | 1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methylpyrimidine-2,4(1H,3H)-dione | 830346-47-9 | C13H10F4N2O2 |
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1-[2-氟-6-(三氟甲基)苄基]-5-碘-6-甲基嘧啶-2,4(1h,3h)-二酮 | 1-[2-fluoro-6-(trifluoromethyl)benzyl]-5-iodo-6-methyl-3H-pyrimidine-2,4-dione | 1150560-54-5 | C13H9F4IN2O2 |
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1-[(反式,反式)-4-乙烯基[1,1-联环己烷]-4-基]-4-甲基苯 | 4-(4-methylphenyl)-4'-vinylbicyclohexane | 155041-85-3 | C21H30 |
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1-[(4-甲氧基苯基)甲基]-1H-吡唑-5-胺 | 1-(4-methoxybenzyl)-1H-pyrazol-5-amine | 3528-45-8 | C11H13N3O |
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1-[(3R,3aS,5R,7aR)-1,1,3-三甲基八氢-1H-茚-5-基]丙烷-2-酮 | N-Formyl Varenicline | 796865-82-2 | C14H13N3O |
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1-[(2-氟苯基)甲基]-1H-吡唑并[3,4-b]吡啶-3-甲亚氨酸甲酯 | methyl 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carbimidate | 304874-06-4 | C15H13FN4O |
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1-[(2'-[(乙氧羰基)氧基]脒基)[1,1-联苯基]-4-基)甲基]-2-乙氧基-1H-苯并咪唑-7-甲酸甲酯 | azilsartan methyl ester | 147403-52-9 | C26H22N4O5 |
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1-N-叔丁氧羰基哌啶-4-硼酸频哪醇酯 | tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)piperidine-1-carboxylate | 1048970-17-7 | C16H30BNO4 |
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1-N-BOC-4-(4-甲基苯磺酰氧甲基)哌啶 | N-tert-butoxycarbonyl-4-(4-toluenesulphonyloxymethyl)piperidine | 166815-96-9 | C18H27NO5S |
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1-Cbz-4-羟甲基哌啶 | benzyl 4-(hydroxymethyl)piperidine-N-carboxylate | 122860-33-7 | C14H19NO3 |
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1-Cbz-4-(Boc-氨基)哌啶-4-甲酸 | 1-((benzyloxy)carbonyl)-4-((tert-butoxycarbonyl)amino)piperidine-4-carboxylic acid | 252720-32-4 | C19H26N2O6 |
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1-Boc-4-羟基-4-(羟基甲基)-哌啶 | tert-butyl 4-hydroxy-4-(hydroxymethyl)piperidine-1-carboxylate | 389889-80-9 | C11H21NO4 |
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1-Boc-4-氟-4-甲酰基哌啶 | tert-butyl 4-fluoro-4-formylpiperidine-1-carboxylate | 614731-09-8 | C11H18FNO3 |
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1-Boc-2-羟基甲基-氮杂丁烷 | tert-butyl 2-(hydroxymethyl)azetidine-1-carboxylate | 174346-82-8 | C9H17NO3 |
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1-Boc-1-甲基肼 | 1-methyl-1-tert-butoxycarbonylhydrazine | 21075-83-2 | C6H14N2O2 |
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1-Boc-1,10-二氨基癸烷 | tert-butyl N-(10-aminodecyl)carbamate | 216961-61-4 | C15H32N2O2 |
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1-BOC-吡咯-2-硼酸频那醇酯 | Tert-butyl 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrrole-1-carboxylate | 1072944-98-9 | C15H24BNO4 |
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1-BOC-3,3-二甲基-4-氧代哌啶 | tert-butyl 3,3-dimethyl-4-oxopiperidine-1-carboxylate | 324769-06-4 | C12H21NO3 |
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1-(邻氯苯基)哌嗪盐酸盐 | 1-(2-chlorophenyl)piperazine hydrochloride | 41202-32-8 | C10H13ClN2*ClH |
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1-(苯并[d][1,3]二氧杂环戊烯-5-基)-2-溴丙烷-1-酮 | 1-(3,4-(methylenedioxy)phenyl)-2-bromopropan-1-one | 52190-28-0 | C10H9BrO3 |
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1-(甲氧基甲基)-3-(三氟甲基)吡唑-4-硼酸 | (1-(Methoxymethyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)boronic acid | 1218790-73-8 | C6H8BF3N2O3 |
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1-(甲基磺酰基)螺[吲哚啉-3,4’-哌啶] | 1-(methylsulfonyl)spiro[indoline-3,4’-piperidine] | 178261-41-1 | C13H18N2O2S |
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1-(环丙基羰基)哌嗪盐酸盐 | cyclopropyl(piperazin-1-yl)methanone hydrochloride | 1021298-67-8 | C8H14N2O*ClH |
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1-(溴甲基)-3-氯-2-硝基苯 | 3-chloro-2-nitrobenzyl bromide | 56433-00-2 | C7H5BrClNO2 |
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1-(溴甲基)-3-氯-2-氟苯 | 1-(bromomethyl)-3-chloro-2-fluorobenzene | 85070-47-9 | C7H5BrClF |
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1-(氟甲基)环丙胺盐酸盐 | 1-(fluoromethyl)cyclopropan-1-amine hydrochloride | 1445951-06-3 | C4H8FN*ClH |
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1-(叔丁氧基羰基)-2-吲哚啉羧酸 | 1-t-butoxycarbonyl-2,3-dihydroindole-2-carboxylic acid | 137088-51-8 | C14H17NO4 |
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1-(乙基磺酰基)-2-硝基-4-(三氟甲基)苯 | ethyl-(2-nitro-4-trifluoromethyl-phenyl)-sulfone | 364-00-1 | C9H8F3NO4S |
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1-(三氟甲基环丙基)苯 | (1-(trifluoromethyl)cyclopropyl)benzene | 883547-73-7 | C10H9F3 |
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1-(beta-羧基乙基)-3,3-二甲基-6'-硝基螺(吲哚啉- 2,2'-2H-苯并吡喃) | 2-(3',3'-dimethyl-6-nitro-3'-H-spiro[chromene-2,2'-indol]-1'-yl)propanoic acid | 55779-26-5 | C21H20N2O5 |
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