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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曲美替尼 | N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide dimethyl sulfoxide solvate | 1187431-43-1 | C2H6OS*C26H23FIN5O4 |
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曲格列汀琥珀酸盐 | trelagliptin succinate | 1029877-94-8 | C4H6O4*C18H20FN5O2 |
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曲前列尼尔中间体 | (1R,2R,3aS,9aS)-1-((S)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]naphthalene-2,5-diol | 101692-02-8 | C21H32O3 |
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普萘洛尔中间体.醚化物 | 8,9-difluoro-5-methyl-6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid | 80076-47-7 | C14H11F2NO3 |
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普拉朵林 | pravadoline | 92623-83-1 | C23H26N2O3 |
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普伐他汀类酯 | pravastatin lactone | 85956-22-5 | C23H34O6 |
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日本前胡醇 | decursinol | 23458-02-8 | C14H14O4 |
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新戊酰基乙腈 | trimethylacetylacetonitrile | 59997-51-2 | C7H11NO |
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拉氧头孢钠中间体 2 | 7β-amino-7α-methoxy-3-(1-methyl-1H-tetrazol-5-ylthiomethyl)-1-oxa-3-cephem-4-carboxylic acid diphenylmethyl ester | 66510-99-4 | C24H24N6O5S |
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抗生素EM 5519 | Safracin B | 82029-27-4 | C28H36N4O7 |
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托利咪酮 | Tolimidone | 41964-07-2 | C11H10N2O2 |
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扎那米韦中间体2 | 5-acetamido-4-amino-2,6-anhydro-3,4,5-trideoxy-D-glycero-D-galacto-non-2-enonic acid | 130525-62-1 | C11H18N2O7 |
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扎那米韦 | methyl 5-acetamido-7,8,9-tri-O-acetyl-4-amino-2,6-anhydro-3,4,5-trideoxy-D-glycero-D-galacto-non-2-enonate | 139110-70-6 | C18H26N2O10 |
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戊-O-乙酰基碘帕醇 | (S)-N,N'-bis[2-ethanoyloxy-1-[(ethanoyloxy)methyl]ethaneyl]-5-[(2-ethanoyloxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide | 289890-55-7 | C27H32I3N3O13 |
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愈创木酚缩水甘油醚 | 2-(2-methoxy-phenoxymethyl)-oxirane | 2210-74-4 | C10H12O3 |
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恶唑-2-甲酸乙酯 | ethyl oxazole-2-carboxylate | 33036-67-8 | C6H7NO3 |
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必索西定 | Bisoxatin | 17692-24-9 | C20H15NO4 |
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德罗特韦中间体 | (4R,12aS)-7-(benzyloxy)-4-methyl-3,4,12,12a-tetrahydro-2H-pyrido[1′,2’:4,5] pyrazino[2,1-b][1,3]oxazine-6,8-dione | 1206102-09-1 | C19H20N2O4 |
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德罗特韦N-4 | methyl 1-(2,2-dihydroxyethyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylate | 1206102-08-0 | C16H17NO6 |
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弗雷拉纳中间体九 | 4-(5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-2-methylbenzoic acid | 864725-62-2 | C18H12Cl2F3NO3 |
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异烟酸乙酯 1-氧化物 | ethyl isonicotinate N-oxide | 14906-37-7 | C8H9NO3 |
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异吲哚啉-5-甲腈 | 5-cyano-2,3-dihydro-1H-isoindole | 263888-58-0 | C9H8N2 |
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异丙氨基比林 | ramifenazone | 3615-24-5 | C14H19N3O |
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异丙基脲 | N-isopropylurea | 691-60-1 | C4H10N2O |
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异丙基肼盐酸盐 | isopropylhydrazine hydrochloride | 16726-41-3 | C3H10N2*ClH |
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异丁芬酸 | ibufenac | 1553-60-2 | C12H16O2 |
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异丁基丙二酸二乙酯 | (2-methylpropyl)-propanedioic acid, diethyl ester | 10203-58-4 | C11H20O4 |
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度鲁特韦中间体-6 | methyl 1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylate | 1206102-07-9 | C17H19NO6 |
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庚酸雌二醇 | 17β-estradiol enanthate | 4956-37-0 | C25H36O3 |
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帕拉米松乙酸酯 | paramethasone acetate | 1597-82-6 | C24H31FO6 |
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帕利哌酮十四酸酯 | paliperidone myristate | 1172995-11-7 | C37H53FN4O4 |
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布酰胺 | Butoctamide | 32838-26-9 | C12H25NO2 |
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巴西芬净 | Basifungin | 127785-64-2 | C60H92N8O11 |
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巴瑞克替尼中间体3 | (4-(1-(3-(cyanomethyl)-1-(ethylsulfonyl)azetidin-3-yl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl pivalate | 1187595-90-9 | C22H27N7O4S |
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己二酸酐 | adipic anhydride | 2035-75-8 | C6H8O3 |
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己二酸单叔丁酯 | 6-(tert-butoxy)-6-oxohexanoic acid | 52221-07-5 | C10H18O4 |
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己二酸 1,6-二(2,5-二氧代-1-吡咯烷基)酯 | bis(2,5-dioxopyrrolidin-1-yl) adipate | 59156-70-6 | C14H16N2O8 |
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左旋-3-溴樟脑 | endo-2-bromocamphor | 76-29-9 | C10H15BrO |
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左乙拉西坦酸 | (R)-2-pyrrolidone-N-butyric acid | 103833-72-3 | C8H13NO3 |
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尼罗替尼单盐酸盐单水合物 | 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide monohydrochloride monohydrate | 923288-90-8 | C28H22F3N7O*ClH*H2O |
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对苯丁氧基苯甲酸 | 4-(4-phenylbutoxy)benzoic acid | 30131-16-9 | C17H18O3 |
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对羟基苯海因 | 5-(4-hydroxy-phenyl)-imidazolidine-2,4-dione | 2420-17-9 | C9H8N2O3 |
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对硝基乙酰苯胺 | N-(4-Nitrophenyl)acetamide | 104-04-1 | C8H8N2O3 |
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对甲苯磺酰脲 | 4-toluenesulfonylurea | 1694-06-0 | C8H10N2O3S |
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对甲氧基肉桂酸甲酯 | 3-methoxybenzyl acrylate | 144261-46-1 | C11H12O3 |
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对特丁基苯肼盐酸盐 | p-tert-butylphenylhydrazine | 61765-93-3 | C10H16N2 |
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对新戊酰氧基苯磺酰氯 | 4-pivaloyloxybenzenesulfonyl chloride | 150374-99-5 | C11H13ClO4S |
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定制在研 | N'-(4-fluorophenyl)-N-(4-((6-hydroxy-7-methoxyquinolin-4-yl)oxy)phenyl)cyclopropane-1,1-dicarboxamide | 1628530-47-1 | C27H22FN3O5 |
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安立生坦酰基beta-D-葡糖苷酸 | Ambrisentan glucuronide | 1106685-58-8 | C28H30N2O10 |
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孟鲁斯特亚砜 | [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methyethyl)phenyl]propyl]sulfinyl]methyl]cyclopropane acetic acid | 1152185-58-4 | C35H36ClNO4S |
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