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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联苯戊酮 | 1-([1,1'-biphenyl]-4-yl)pentan-1-one | 42916-73-4 | C17H18O |
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羟基硫胺素盐酸盐 | oxythiamine chloride hydrochloride | 614-05-1 | C12H16N3O2S*ClH*Cl |
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美雄醇 | methylandrostenediol | 521-10-8 | C20H32O2 |
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美替诺龙庚酸酯 | methenolone enanthate | 303-42-4 | C27H42O3 |
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美司那 | 2-Mercaptoethanesulfonic acid sodium | 19767-45-4 | C2H6NaO3S2 |
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美卡比酯 | mecarbinate | 15574-49-9 | C13H15NO3 |
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美他法仑 | L-m-sarcolysin | 1088-80-8 | C13H18Cl2N2O2 |
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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 |
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罗沙司他N-1 | methyl 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido) acetate | 1421312-36-8 | C20H18N2O5 |
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罗替戈汀中间体 | (S)-(-)-5-hydroxy-2-(n-propylamino)tetralin hydrobromide | 165950-84-5 | BrH*C13H19NO |
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维贝格龙 | vibegron | 1190389-15-1 | C26H28N4O3 |
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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 |
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维生素C磷酸酯 | L-ascorbic acid 2-phosphate | 23313-12-4 | C6H9O9P |
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维洛沙秦 | viloxazine | 46817-91-8 | C13H19NO3 |
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维兰特罗三苯乙酸盐 | vilanterol trifenatate | 503070-58-4 | C20H16O2*C24H33Cl2NO5 |
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维兰特罗 | vilanterol | 503068-34-6 | C24H33Cl2NO5 |
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红霉素A肟 | erythromycin A oxime | 13127-18-9 | C37H68N2O13 |
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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 |
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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 |
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糠酸氟替卡松 | fluticasone furoate | 397864-44-7 | C27H29F3O6S |
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粪卟啉I二盐酸盐 | Coproporphyrin I dihydrochloride | 69477-27-6 | C36H40Cl2N4O8 |
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米酵菌酸 | bongkrekic acid | 11076-19-0 | C28H38O7 |
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米氮平酸 | 2-(4-methyl-2-phenyl-1-piperazinyl)-3-pyridinecarboxylic acid | 61338-13-4 | C17H19N3O2 |
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米拉贝隆中间体 | (R)-2-hydroxy-N-(4-nitrophenethyl)-2-phenylacetamide | 521284-19-5 | C16H16N2O4 |
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米拉贝隆中间体 | (R)-2-[ [2-(4-aminophenyl)ethyl]-amino]-1-phenylethanol monohydrochloride | 521284-22-0 | C16H20N2O*ClH |
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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 |
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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 |
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磺胺琥珀酸 | 4-oxo-4-((4-sulfamoylphenyl)amino)butanoic acid | 3563-14-2 | C10H12N2O5S |
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磷酸鲁索替尼 | ruxolitinib phosphate | 1092939-17-7 | C17H18N6*H3O4P |
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磷酸红霉素 | Erythromycin Phosphate | 4501-00-2 | C37H70NO17P |
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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 |
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磷酸二叔丁酯钾盐 | Di-tert-butyl hydrogen phosphate; potassium salt | 33494-80-3 | C8H19KO4P |
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磷酰胆碱氯化钙盐 | Phosphocholine chloride calcium salt tetrahydrate | 15557-11-6 | C5H21CaClNO8P |
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磷康唑 | Fosfluconazole | 194798-83-9 | C13H13F2N6O4P |
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碘甲基舒巴坦 | iodomethyl 1,1-dioxopenicillanate | 76247-39-7 | C9H12INO5S |
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碘代对苯二甲酸二甲酯 | dimethyl 2-iodoterephthalate | 165534-79-2 | C10H9IO4 |
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硫代西地那非 | 5-[2-ethoxy-5-(4-methyl-piperazine-1-sulfonyl)-phenyl]-1-methyl-3-propyl-1,6-dihydro-pyrazolo[4,3-d]pyrimidine-7-thione | 479073-79-5 | C22H30N6O3S2 |
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硫代吗啉 | Thiomorpholin | 123-90-0 | C4H9NS |
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盐酸环己胺 | cyclohexylamine hydrochloride | 4998-76-9 | C6H14N*Cl |
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盐酸恩诺沙星 | Enrofloxacin hydrochloride | 93106-59-3 | C19H22FN3O3*ClH |
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盐酸左美托咪定 | dexmedetomidine hydrochloride | 190000-46-5 | C13H16N2*ClH |
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盐酸利莫那班 | rimonabant hydrochloride | 158681-13-1 | C22H21Cl3N4O*ClH |
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盐酸二乙氨基乙醇 | 2-(Diethylamino)ethenol hydrochloride | 13989-32-7 | C6H16ClNO |
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甲磺酸帕苏沙星 | 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, methanesulfonate (1:1) | 136905-87-8 | C17H19FN2O7S |
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甲磺酸5-[2-(二氨基甲亚基)肼基<联氨基>]-6-羟基-1-甲基-3-羰基-3H-吲哚正离子 | 2-{[4-(m-tolylazo)-m-tolyl]azo}-p-cresol | 2475-42-5 | C21H20N4O |
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甲硫美芬铵 | Mefenidramium metilsulfate | 4858-60-0 | C19H27NO5S |
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甲状腺素酰基-β-D-葡糖醛酸 | Levothyroxine Acyl Glucuronide | 909880-81-5 | C21H19I4NO10 |
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甲烷磺酸[9,9-二甲基-4,5-双(二苯基膦)呫吨][2-氨基-1,1-联苯]钯(II)二氯 | xantphos-Pd-G3 | 1445085-97-1 | C52H45NO4P2PdS |
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甲基硫雄甾醇代谢物 | 2,3-Thioepoxy madol | 4267-80-5 | C20H32OS |
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甲基硫代乙酸甲酯 | methyl 2-(methylthio)acetate | 16630-66-3 | C4H8O2S |
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