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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N-苯甲酰基-5’-O-(4,4-二甲氧基三苯甲基)-2’-O-[(叔丁基)二甲基硅基]腺苷-3’-(2-氰基乙基-N,N-二异丙基)亚磷酰胺 | N<sup>6</sup>-benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-O-(tert-butyldimethylsilyl)adenosine 3'-O-(2-cyanoethyl N,N-diisopropylphosphoramidite) | 104992-55-4 | C53H66N7O8PSi |
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N-苯甲酰基-5'-O-[二(4-甲氧基苯基)苯基甲基]-2'-脱氧-5-甲基胞苷 | 5'-O-(4,4'-dimethoxytriphenylmethyl)-2'-deoxy-N<sup>4</sup>-benzoyl-5-methylcytidine | 104579-03-5 | C38H37N3O7 |
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N-苯甲酰基-5'-O-[二(4-甲氧基苯基)苯基甲基]-2'-脱氧-2'-氟腺苷3'-[2-氰基乙基N,N-二异丙基氨基亚磷酸酯] | (2R,3R,4R,5R)-5-(6-benzamido-9H-purin-9-yl)-2-((bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-4-fluorotetrahydrofuran-3-yl (2-cyanoethyl) diisopropylphosphoramidite | 136834-22-5 | C47H51FN7O7P |
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N-苯基吲哚酮 | 1-phenyl-1,3-dihydro-indol-2-one | 3335-98-6 | C14H11NO |
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N-苄氧羰基-L-丝氨酰基甘氨酸 | N-benzyloxycarbonylserylglycine | 30735-20-7 | C13H16N2O6 |
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N-苄基-2-硝基苯磺酰胺 | N-benzyl-2-nitrobenzenesulfonamide | 42060-32-2 | C13H12N2O4S |
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N-芴甲氧羰基-L-谷氨酸 1-烯丙基酯 | Nα-(9-fluorenylmethoxycarbonyl)-L-glutamic acid α-allyl ester | 144120-54-7 | C23H23NO6 |
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N-芴甲氧羰基-5-氟-L-色氨酸 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3-(5-fluoro-1H-indol-3-yl)propanoic acid | 908846-88-8 | C26H21FN2O4 |
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N-硫酰胺基-3-氯丙脒盐酸盐 | N-sulfamyl-(3-chloro)-propionamidine hydrochloride | 106649-95-0 | C3H8ClN3O2S*ClH |
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N-甲酰基-D-亮氨酸 (1S)-1-[[(2S,3S)-3-己基-4-氧代-2-氧杂环丁基]甲基]十二烷基酯 | N-formyl-D-leucine-(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester | 104872-28-8 | C29H53NO5 |
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N-甲酰基-D-亮氨酸 (1R)-1-[[(2R,3R)-3-己基-4-氧代-2-氧杂环丁基]甲基]十二烷基酯 | (R)-1-((2R,3R)-3-hexyl-4-oxooxetan-2-yl)tridecan-2-yl formyl-D-leucinate | 104872-27-7 | C29H53NO5 |
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N-甲氧基-N-甲基-苯乙酰胺 | N-methoxy-N-methylphenylacetamide | 95092-10-7 | C10H13NO2 |
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N-甲基环己胺 | N-methyl-N-cyclohexylamine | 100-60-7 | C7H15N |
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N-甲基-N-(3-[((N-叔丁氧羰基-N-甲基氨基)乙酰氧基)甲基]吡啶-2-基)氨基甲酸(1-氯乙基)酯 | N-methyl N-(3-[((N-tert-butoxycarbonyl-N-methylamino)acetoxy)methyl]pyridin-2-yl)carbamic acid (1-chloroethyl) ester | 338990-31-1 | C18H26ClN3O6 |
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N-甲基-N-((3R,4R)-4-甲基哌啶-3-基)-7H-吡咯并[2,3-D]嘧啶-4-胺 | N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine | 477600-74-1 | C13H19N5 |
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N-甲基-2-吡咯腈 | 1-methyl-1H-pyrrole-2-carbonitrile | 34884-10-1 | C6H6N2 |
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N-甲基-1-萘甲胺 | N-methyl-1-naphthalenemethylamine | 14489-75-9 | C12H13N |
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N-琥珀酰亚胺碳酸叔丁酯 | tert-butyl 2,5-dioxopyrrolidin-1-yl carbonate | 13139-12-3 | C9H13NO5 |
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N-环丙基-甲酰胺 | N-cyclopropylformamide | 58644-54-5 | C4H7NO |
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N-牛脂基-1,3-丙撑二胺 | N'-ethylpropane-1,3-diamine | 61791-55-7 | C10H28N4 |
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N-烯丙基咪唑 | 1-allylimidazole | 31410-01-2 | C6H8N2 |
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N-氨基-3-氮杂双环[3.3.0]辛烷盐酸盐 | N-amino-3-azabicyclo[3,3,0]octane hydrochloride | 58108-05-7 | C7H14N2*ClH |
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N-对甲苯磺酰甲基甲酰胺 | N-(tosylmethyl)formamide | 36635-56-0 | C9H11NO3S |
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N-叔丁氧羰基-4-[二(2-羟基乙基)氨基]-L-苯基丙氨酸甲酯 | Methyl 4-[bis(2-hydroxyethyl)amino]-N-(tert-butoxycarbonyl)-D-phenylalaninate | 1217651-06-3 | C19H30N2O6 |
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N-叔丁氧羰基-(S)-2-吗啉甲醇 | tert-butyl (2S)-2-(hydroxymethyl)morpholine-4-carboxylate | 135065-76-8 | C10H19NO4 |
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N-叔丁基-4-硝基苯磺酰胺 | N-dimethylethyl-4-nitrobenzenesulfonamide | 49690-09-7 | C10H14N2O4S |
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N-去甲酰基-N-特戊酰奥利司他 | N-Deformyl-N-pivaloyl Orlistat | 1356017-35-0 | C33H61NO5 |
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N-亚硝基普萘洛尔 | N-nitrosopropranolol | 84418-35-9 | C16H20N2O3 |
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N-二苯甲基氮杂环丁烷-3-醇 | 1-(diphenylmethyl)-3-hydroxyazetidine | 18621-17-5 | C16H17NO |
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N-乙酰基-L-酪氨酰-L-精氨酸十六烷基酯 | Acetyl dipeptide-1 cetyl ester | 196604-48-5 | C33H57N5O5 |
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N-乙酰基-L-半胱氨酸甲酯 | Ac-Cys-OMe | 7652-46-2 | C6H11NO3S |
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N-乙酰基-3-乙酰氧基-5-苯基吡咯 | 1-acetyl-5-phenyl-1H-pyrrol-3-yl acetate | 100750-39-8 | C14H13NO3 |
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N-乙酰基-2'-O-甲基胞苷 | N<sup>4</sup>-acetyl-2'-O-methyl cytidine | 113886-71-8 | C12H17N3O6 |
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N-乙酰-D-苯丙氨酸 | (R)-N-acetylphenylalanin | 10172-89-1 | C11H13NO3 |
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N-乙基羟胺盐酸盐 | N-ethylhydroxylamine hydrochloride | 42548-78-7 | C2H8NO*Cl |
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N-乙基-N-3-((3-二甲氨基-1-氧代-2-丙烯基)苯基)乙酰胺 | N-{3-[3-(dimethylamino)prop-2-enoyl]phenyl}-N-ethylacetamide | 96605-66-2 | C15H20N2O2 |
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N-丁基-N-乙基-2,5,6-三甲基-7-(2,4,6-三甲基苯基)-7H-吡咯并[2,3-d]嘧啶-4-胺单盐酸盐 | Antalarmin hydrochloride | 220953-69-5 | C24H35ClN4 |
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N-{[(1S,2S,10R,12S,13S)-12,18-二羟基-7,17-二甲氧基-6,16,21-三甲基-5,8-二氧代-11,21-二氮杂五环[11.7.1.02,11.04,9.015,20]二十一-4(9),6,15,17,19-五烯-10-基]甲基}-L-丙氨酰胺 | safracin B | 87578-99-2 | C28H36N4O7 |
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N-[苯胺基(苯氧基)磷酰基]苯胺 | phenyl dianilidophosphate | 18995-02-3 | C18H17N2O2P |
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N-[芴甲氧羰基]-4-[[[(4S)-六氢-2,6-二氧代-4-嘧啶基]羰基]氨基]-L-苯丙氨酸 | Fmoc-Aph(Hor)-OH | 1253282-31-3 | C29H26N4O7 |
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N-[[2-[[[4-(氨基亚氨基甲基)苯基]氨基]甲基]-1-甲基-1H-苯并咪唑-5-基]羰基]-n-(2-吡啶)-beta-丙氨酸乙酯盐酸盐 | ethyl 3-(2((4-carbamimidoylphenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate hydrochloride | 211914-50-0 | C27H29N7O3*ClH |
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N-[5-[(4-甲基苯基)磺酰基]-5H-吡咯并[2,3-B]吡嗪-2-基]氨基甲酸乙酯 | ethyl (5-tosyl-5H-pyrrolo[2,3-b]pyrazin-2-yl)carbamate | 1869118-24-0 | C16H16N4O4S |
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N-[4-(氨基磺酰基)苄基]乙酰胺 | N-(4-sulfamoylbenzyl)acetamide | 2015-14-7 | C9H12N2O3S |
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N-[4-(2,5-二氢-5-氧代-1,2,4-恶二唑-3-基)苯基]甘氨酸 | 2-[4-(1,2,4-oxadiazol-5-one-3-yl)-phenylamino]-acetic acid | 872728-82-0 | C10H9N3O4 |
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N-[3-氟-4-[6-(2-甲基-2H-四唑-5-基)-3-吡啶基]苯基]氨基甲酸苄酯 | 3-fluoro-4-(6-(2-methyl-2H-tetrazole-5-yl)pyridin-3-yl)phenyl-carbamic acid benzylester | 1220910-89-3 | C21H17FN6O2 |
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N-[3-氟-4-[(甲基氨基)羰基]苯基]-2-甲基丙氨酸 | 2-(3-fluoro-4-methylcarbamoyl-phenylamino)-2-methyl-propionic acid | 1289942-66-0 | C12H15FN2O3 |
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N-[3-氟-4-[(甲基氨基)羰基]苯基]-2-甲基-丙氨酸甲酯 | N-[3-fluoro-4-[(methylamino)carbonyl]phenyl]-2-methylalanine methyl ester | 1332524-01-2 | C13H17FN2O3 |
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N-[3-[[3-环丙基-1-(2-氟-4-碘苯基)-1,2,3,4,7,8-六氢-6,8-二甲基-2,4,7-三氧代吡啶并[2,3-d]嘧啶-5-基]氨基]苯基]乙酰胺 | N-{3-[3-cyclopropyl-1-(2-fluoro-4-iodophenyl)-6,8-dimethyl-2,4,7-trioxo-1,2,3,4,7,8-hexahydropyrido[2,3-d]pyrimidin-5-ylamino]phenyl}acetamide | 871700-25-3 | C26H23FIN5O4 |
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N-[3-[5-(4-氯苯基)-1-(2,6-二氯苯甲酰基)-1H-吡咯并[2,3-b]吡啶-3-基)羰基]-2,4-二氟苯基]-1-丙烷磺酰胺 | propane-1-sulfonic acid {3-[5-(4-chlorophenyl) 1-(2,6-dichloro-benzoyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide | 1262985-23-8 | C30H20Cl3F2N3O4S |
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N-[3-[(5-溴-1H-吡咯并[2,3-b]吡啶-3-基)羰基]-2,4-二氟苯基]-1-丙烷磺酰胺 | N-(3-(5-bromo-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide | 918504-27-5 | C17H14BrF2N3O3S |
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