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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—— | ZINC;12-hydroxyoctadec-9-enoate | 13040-19-2 | C36H66O6Zn |
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—— | 1,5-Methano-11H-furo(3,2-g)pyrano(3,2-b)xanthene-3a(4H)-crotonaldehyde, 1,2,5,7-tetrahydro-8-hydroxy-alpha,2,2,11,11-pentamethyl-13-(3-methyl-2-butenyl)-4,7-dioxo-, trans- | 1183-12-6 | C33H36O7 |
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—— | momelotinib dimesylate | 1056636-07-7 | 2CH4O3S*C23H22N6O2 |
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—— | (2S)-1-[(Benzyloxy)carbonyl]azetidine-2-carboxylate | 25654-52-8 | C12H12NO4- |
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—— | (2S,3Z)-5-{[(2R,3R,5S,6S)-2,5-dimethyl-6-{(2E,4E)-3-methyl-5-[(3R,4R,5R,7S,8R)-4,7,8-trihydroxy-7-methyl-1,6-dioxaspiro[2.5]oct-5-yl]penta-2,4-dien-1-yl}tetrahydro-2H-pyran-3-yl]amino}-5-oxopent-3-en-2-yl acetate | 146478-73-1 | C27H41NO9 |
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—— | Di(p-tolylidene)sorbitol | 54686-97-4 | C22H26O6 |
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—— | (2S,3R,5R)-5-Chloro-2-(((4-chlorobenzoyl)oxy)methyl)tetrahydrofuran-3-yl 4-chlorobenzoate | 21740-23-8 | C19H15Cl3O5 |
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—— | (1R,3s,5S)-8-Benzyl-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octane | 423165-13-3 | C20H28N4 |
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—— | 3-[N-(p-chlorobenzyl)-3-(3,3-dimethyl-1-oxo-1-butyl)-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid | 136668-50-3 | C36H37ClN2O4 |
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—— | ((3SR,4SR)-1-tert-butoxycarbonyl)4-(ethoxycarbonyl)pyrrolidine-3-carboxylic acid | 252919-44-1 | C13H21NO6 |
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—— | 1,3,5-CYCLOHEXANETRICARBONITRILE | 168280-46-4 | C9H9N3 |
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—— | [3H]-(–)-2-b-carbomethoxy-3-b-(4-fluorophenyl)tropane. | 50370-56-4 | C16H20FNO2 |
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—— | 1,2-difluoro-3-((4-fluoro-2-methoxy-5-nitrophenoxy)methyl)-4-methoxybenzene | 1073435-71-8 | C15H12F3NO5 |
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—— | benzhydryl 3-hydroxy-7β-(α-phenylacetamido)-3-cephem-4-carboxylate | 54639-48-4 | C28H24N2O5S |
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—— | 4,5-bis(2-methoxyethoxy)benzene-1,2-diamine | 344438-55-7 | C12H20N2O4 |
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—— | ((3aR,5R,6S,6aR)-5-((tert-butyldiphenylsilyloxy)methyl)-2,2-dimethyl-6-(naphthalen-2-ylmethoxy)-dihydro-5H-furo[3,2-d][1,3]dioxol-5-yl)methanol | 956485-08-8 | C36H42O6Si |
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—— | (S)-Viloxazine Hydrochloride | 56287-61-7 | C13H20ClNO3 |
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—— | Morpholine, 2-[[2-(ethoxy-d5)phenoxy]methyl]- | 117320-32-8 | C13H19NO3 |
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—— | methyl (S)-(-)-2,3,4,9-tetrahydro-1H-pyrido<3,4-b>indole-3-carboxylate hydrochloride | 83159-19-7 | C13H14N2O2*ClH |
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—— | (E)-3-(dimethylamino)-1-mesitylprop-2-en-1-one | 78830-43-0 | C14H19NO |
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—— | Bis-(dibenzo<d,f>-1,3,2λ<sup>3</sup>-dioxaphosphepino)-2,2'-dioxobiphenyl | 122605-42-9 | C36H24O6P2 |
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—— | Δ<sup>5,7</sup>-Pregnen-3,20-diethylenketal | 5488-51-7 | C25H36O4 |
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—— | 6-Cyanbenzo<b>thiophen-2-carbonsaeure-ethylester | 105191-16-0 | C12H9NO2S |
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—— | 3-Ethylenolether von Androst-4-en-3.17-dion | 972-46-3 | C21H30O2 |
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—— | diethyl cyclohexane 1,3-dicarboxylate | 72903-26-5 | C12H20O4 |
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—— | (E)-3-(benzo[d][1,3]dioxol-5-yl)-N-propylacrylamide | 116591-96-9 | C13H15NO3 |
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—— | Bicyclo[4.1.0]heptan-2-amine | 78293-48-8 | C7H13N |
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—— | ethyl {4-amino-3-[(3-chloro-5-cyanophenyl)oxy]-2-fluorophenyl}acetate | 770719-11-4 | C17H14ClFN2O3 |
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—— | 1,1-dicyano-4-(N,N-dimethylamino)-2-methoxy-1,3-butadiene | 95689-38-6 | C9H11N3O |
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—— | (8R,9R,13S,14R,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,4,6,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one | 1095-74-5 | C21H28O2 |
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—— | 5,5-dimethyl-1,3,2-dioxathiane-2,2-dioxide | 1755-97-1 | C5H10O4S |
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—— | methanesulfonic acid 2-[2-methyl-5-(4-methylsulfanylphenyl)pyrrol-1-yl]ethyl ester | 494850-87-2 | C15H19NO3S2 |
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—— | 2-amino-5-iodo-3-chlorobenzoic acid | 101012-31-1 | C7H5ClINO2 |
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—— | (+/-)-trans-2-fluorocyclohexylamine | 1039741-13-3 | C6H12FN |
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—— | 3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)-acrylic acid | 133262-97-2 | C17H15ClO4 |
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—— | 5-chloro-2-fluoro-N-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)phenyl]benzenesulfonamide | 1428182-88-0 | C18H20BClFNO4S |
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—— | Erythromycin, 9-oxime | 13127-18-9 | C37H68N2O13 |
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—— | Pregnenolon-3β-sulfonsaeureester | 1247-64-9 | C21H32O5S |
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—— | Pregnenolon-sulfat | 1247-64-9 | C21H32O5S |
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—— | Cis-di-tert-butyl-cyclopent-4-ene-1,3-diyl dicarbonate | 890122-43-7 | C15H24O6 |
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—— | 17β-cyano-3,3-[1,2-ethanediylbis(oxy)]-17α-trimethylsilyloxyestra-5(10),9(11)-diene | 54690-63-0 | C24H35NO3Si |
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—— | (2S)-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]pent-4-enoic acid | 136092-76-7 | C11H19NO4 |
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—— | N-(5-amino-2-chloro-4-fluoro-benzoyl)-N'-methyl-N'-isopropylsulfamide | 685568-49-4 | C11H15ClFN3O3S |
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—— | MIND4-19 | 129544-85-0 | C22H19N3OS |
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—— | Adavelt | 1961312-55-9 | C27H26F2N2O6 |
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—— | 4-hydroxy-2-oxo-2H-coumarin-3-yl styryl ketone | 209973-90-0 | C18H12O4 |
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—— | 2-propenamide, N-[2-hydroxy-2-(4-methoxyphenyl)ethyl]-3-phenyl-, (2E) | 456-12-2 | C18H19NO3 |
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—— | 4-methoxy-dibenzofuran-1-ylamine | 685873-83-0 | C13H11NO2 |
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—— | AZ7550 | 1421373-99-0 | C27H31N7O2 |
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—— | 4-mesitylaniline | 66818-61-9 | C15H17N |
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