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原料药中间体

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:

  1. 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。

  2. 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。

  3. 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。

  4. 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。

  5. 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。

下级分类

中文名称 英文名称 CAS号 化学式
艾地骨化醇90A-环 ((Z)-2-((3R,4R,5R)-3,5-bis((tert-butyldimethylsilyl)oxy)-4-(3-((tert-butyldiphenylsilyl) oxy)propoxy)-2-methylenecyclohexylidene)ethyl)diphenylphosphine oxide 1254276-84-0 C52H75O5PSi3
艾乐替尼中间体 2-(4-ethyl-3-iodophenyl)-2-methylpropionic acid 1256584-73-2 C12H15IO2
艾乐替尼中间体 6-cyano-2-{2-[4-ethyl-3-(4-(morpholin-4-yl)piperidin-1-yl)phenyl]propan-2-yl}-1H-indole-3-carboxylic acid 1256584-78-7 C30H36N4O3
色酚 AS-BI 5-(2'-Hydroxy-3'-naphthoyl-amino)benzimidazol-2-one 26848-40-8 C18H13N3O3
舒巴坦杂质19 benzhydryl 2-[4-(2-benzothiazolyldithio)-2-oxoazetidinyl-1]-2-(isopropyl)acetate 87579-79-1 C28H24N2O3S3
膦酸,[2-(2-甲基-1,3-二噁戊环-2-基)-2-羰基乙基]-(9CI) endo-Bicyclo<2,2,1>-hepten-(2)-carbonsaeure-(5)-methylester 769-85-7 C9H12O2
膦酸,[2-(2-甲基-1,3-二噁戊环-2-基)-2-羰基乙基]-(9CI) methyl (1S,2R,4S)-bicyclo[2.2.1]hept-5-ene-2-carboxylate 769-85-7 C9H12O2
腺苷酰基-(3,’5’)-胞苷 Cytidin-(3',5')-adenosin 2382-66-3 C19H25N8O11P
腺苷酰-(3'→5')-胞苷 Adenylyl cytidine 4833-63-0 C19H25N8O11P
脱氢诺龙醋酸酯 6-dehydro-19-nortestosterone acetate 2590-41-2 C20H26O3
脯氨酰-甘氨酰-脯氨酰-肾上腺皮质激素 (4-7) H-Met-Glu-His-Phe-Pro-Gly-Pro 80714-61-0 C37H51N9O10S
胞苷酰-(5'->3')-鸟苷 Phosphoric acid (2R,3S,4R,5R)-5-(2-amino-6-oxo-1,6-dihydro-purin-9-yl)-4-hydroxy-2-hydroxymethyl-tetrahydro-furan-3-yl ester (2R,3S,4R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl ester 4785-04-0 C19H25N8O12P
胆酸杂质 7,12-dioxolitocholic acid 517-33-9 C24H36O5
胆甾醇硫酸盐 cholesterol 3-sulfate 1256-86-6 C27H46O4S
联苯戊酮 1-([1,1'-biphenyl]-4-yl)pentan-1-one 42916-73-4 C17H18O
群勃龙庚酸酯 Trenbolone Enanthate 1629618-98-9 C25H34O3
羟基硫胺素盐酸盐 oxythiamine chloride hydrochloride 614-05-1 C12H16N3O2S*ClH*Cl
美雄醇 methylandrostenediol 521-10-8 C20H32O2
美沙拉嗪EP杂质P 5-amino-2-hydroxy-4'-sulfo-[1,1'-biphenyl]-3-carboxylic acid 887256-40-8 C13H11NO6S
美替诺龙庚酸酯 methenolone enanthate 303-42-4 C27H42O3
美司那 2-Mercaptoethanesulfonic acid sodium 19767-45-4 C2H6NaO3S2
美卡比酯 mecarbinate 15574-49-9 C13H15NO3
美他法仑 L-m-sarcolysin 1088-80-8 C13H18Cl2N2O2
罗红霉素钙盐(链霉菌属载体) 10,16-Docosadienoic acid,11,19,21-trihydroxy-4,6,8,12,14,18,20-heptamethyl-22-[(2S,2'R,5S,5'S)-octahydro-5'-[(1R)-1-hydroxyethyl]-2,5'-dimethyl[2,2'-bifuran]-5-yl]-9-oxo-, calcium salt (1:1), (4R,6S,8S,10Z,12R,14R,16E,18R,19R,20S,21S)- 56092-82-1 C41H72CaO9
罗沙司他N-1 methyl 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido) acetate 1421312-36-8 C20H18N2O5
罗替戈汀中间体 (S)-(-)-5-hydroxy-2-(n-propylamino)tetralin hydrobromide 165950-84-5 BrH*C13H19NO
维贝格龙 vibegron 1190389-15-1 C26H28N4O3
维罗非尼中间体 N-(3-(5-bromo-1-(2,6-dichlorobenzoyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide 1262985-24-9 C24H16BrCl2F2N3O4S
维生素C磷酸酯 L-ascorbic acid 2-phosphate 23313-12-4 C6H9O9P
维洛沙秦 viloxazine 46817-91-8 C13H19NO3
维兰特罗三苯乙酸盐 vilanterol trifenatate 503070-58-4 C20H16O2*C24H33Cl2NO5
维兰特罗 vilanterol 503068-34-6 C24H33Cl2NO5
维他命 K1 2,3-环氧化物 vitamin K epoxide 25486-55-9 C31H46O3
纽莫康定 B0 (10S,12R)-N-[(3R,6R,9R,11S,15R,18R,20S,21S,24R,25R)-3-[(1S)-3-amino-1-hydroxy-3-oxopropyl]-6-[(1R,2R)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-11,20,21,25-tetrahydroxy-15-[(1S)-1-hydroxyethyl]-2,5,8,14,17,23-hexaoxo-1,4,7,13,16,22-hexazatricyclo[22.3.0.09,13]heptacosan-18-yl]-10,12-dimethyltetradecanamide 135575-42-7 C50H80N8O17
红霉素A肟 erythromycin A oxime 13127-18-9 C37H68N2O13
索芬胺 1-(5-amino-2,4-dichlorophenyl)-4,5-dihydro-4-difluoromethyl-3-methyl-1,2,4-triazol-5(1H)-one 111992-18-8 C10H8Cl2F2N4O
糠酸莫米松水合物 [(8S,9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] furan-2-carboxylate;hydrate 141646-00-6 C27H32Cl2O7
糠酸氟替卡松 fluticasone furoate 397864-44-7 C27H29F3O6S
粪卟啉I二盐酸盐 Coproporphyrin I dihydrochloride 69477-27-6 C36H40Cl2N4O8
米酵菌酸 bongkrekic acid 11076-19-0 C28H38O7
米氮平酸 2-(4-methyl-2-phenyl-1-piperazinyl)-3-pyridinecarboxylic acid 61338-13-4 C17H19N3O2
米拉贝隆中间体 (R)-2-hydroxy-N-(4-nitrophenethyl)-2-phenylacetamide 521284-19-5 C16H16N2O4
米拉贝隆中间体 (R)-2-[ [2-(4-aminophenyl)ethyl]-amino]-1-phenylethanol monohydrochloride 521284-22-0 C16H20N2O*ClH
科立内酯 (3aR,4S,5R,6aS)-4-(hydroxymethyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one 69222-61-3 C13H20O5
磺达肝癸钠中间体-N-3 methyl O-(2-azido-3,4-di-O-benzyl-2-deoxy-α-D-glucopyranosyl)-(1→4)-O-(2,3-di-O-benzyl-β-D-glucopyranosyl uronic acid)-(1→4)-O-(2-azido-2-deoxy-α-D-glucopyranosyl)-(1→4)-O-(3-O-benzyl-α-L-idopyranosyluronic acid)-(1→4)-2-benzyloxy carbonylamino-3-benzyl-2-deoxy-α-D-glucopyranoside 114903-05-8 C81H91N7O27
磺达肝癸钠中间体 methyl 6-O-acetyl-3-O-benzyl-2-benzyloxycarbonylamino-2-deoxy-4-O-(methyl 2-O-acetyl-3-O-benzyl-α-L-idopyranosyluronate)-α-D-glucopyranoside 114869-97-5 C40H47NO15
磺胺琥珀酸 4-oxo-4-((4-sulfamoylphenyl)amino)butanoic acid 3563-14-2 C10H12N2O5S
磷酸鲁索替尼 ruxolitinib phosphate 1092939-17-7 C17H18N6*H3O4P
磷酸红霉素 Erythromycin Phosphate 4501-00-2 C37H70NO17P
磷酸奥司他韦中间体十一步 ethyl (3R,4R,5S)-4-N-acetyl(1,1-dimethylethyl)amino-5-N,N-diallylamino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate hydrochloride 651324-08-2 C26H44N2O4*ClH