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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—— | 3,20-Bis(ethylenedioxy)pregna-5,7-diene | 19592-55-3 | C25H36O4 |
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—— | [1,1'-Bianthracene]-3,3'-disulfonic acid, 4,4'-diamino-9,9',10,10'-tetrahydro-9,9',10,10'-tetraoxo-, disodium salt | 6022-22-6 | C28H14N2Na2O10S2 |
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—— | 7-Amino-3-[(5-methyl-1,3,4-thiadiazol-2-YL)thiomethyl]cephalosphoranic acid | 30246-33-4 | C11H12N4O3S3 |
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—— | 2,4,6-tris(bromomethyl)-s-triazine | 30361-99-0 | C6H6Br3N3 |
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—— | (2S,4R,8S,12S)-8-acetyl-6,9,13-trimethyl-6-phenyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one | 24356-94-3 | C29H36O4 |
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—— | N-Fmoc-(L)-tyrosine methyl ester | 1270300-64-5 | C25H23NO5 |
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—— | ACP-105 | 899821-23-9 | C16H19ClN2O |
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—— | 1-(3-aminophenyl)-2,2,2-trifluoroethanol | 17556-38-6 | C8H8F3NO |
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—— | 3(2H)-Pyridazinone, 6-(m-methoxyphenyl)-4-methyl-2-(2-morpholinoethyl)-, hydrochloride | 13299-99-5 | C18H24ClN3O3 |
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—— | Bromadol HCL BDPC | 77239-98-6 | C22H28BrNO |
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—— | 5,7,12,14-tetrahydro-5,7,12,14-tetraazapentacene | 162039-67-0 | C18H14N4 |
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—— | bis-1,3-(4-aminobenzamido)benzene | 2362-25-6 | C20H18N4O2 |
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—— | 5-chloropyridin-3-yl 1H-indole-4-carboxylate | 1087243-14-8 | C14H9ClN2O2 |
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—— | (+/-)-coronaridine | 467-77-6 | C21H26N2O2 |
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—— | Cytidine, 2'-deoxy-5-fluoro- | 10356-76-0 | C9H12FN3O4 |
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—— | 2-fluoro-4-methoxy-1-(trifluoromethyl)benzene | 1214344-33-8 | C8H6F4O |
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—— | ethyl 3-amino-7-bromo-1,6-naphthyridine-2-carboxylate | 1620239-76-0 | C11H10BrN3O2 |
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—— | 8-Bromo-9-pentofuranosyl-9H-purine-2,6-diol | 686300-33-4 | C10H11BrN4O6 |
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—— | (-)-Tabernemontanine | 2134-98-7 | C21H26N2O3 |
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—— | 2-Fluoro-9-(2,3,5-tri-o-acetylpentofuranosyl)-9h-purin-6-amine | 15811-32-2 | C16H18FN5O7 |
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—— | (±)-2-(methylaminomethyl)-3,4-dihydro-2H-naphthalen-1-one | 403860-66-2 | C12H15NO |
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—— | 3,5-Bis-o-(4-chlorobenzoyl)-2-deoxypentofuranosyl chloride | 21740-23-8 | C19H15Cl3O5 |
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—— | 4-Amino-8-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-oxopyrido[2,3-d]pyrimidine-6-carboxamide | 36707-00-3 | C13H15N5O6 |
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—— | (1S,3R,4R,6S,7S)-3-(6-N-benzoyladenin-9-yl)-7-[2-cyanoethoxy(diisopropylamino)phosphinoxy]-1-(4,4'-dimethoxytrityloxymethyl)-6-methyl-2,5-dioxabicyclo[2.2.1]heptane | 1197033-19-4 | C49H54N7O8P |
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—— | (1S,3R,4R,6S,7S)-7-[2-cyanoethoxy(diisopropylamino)phosphinoxy]-1-(4,4'-dimethoxytrityloxymethyl)-6-methyl-3-(thymin-1-yl)-2,5-dioxabicyclo[2.2.1]heptane | 1197033-22-9 | C42H51N4O9P |
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—— | (-)-methyl (1S,2S,3R,4R)-3-[(1S)-1-(acetylamino)-2-ethylbutyl]-4-amino-2-hydroxycyclopentanecarboxylate | 229615-05-8 | C15H28N2O4 |
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—— | 4-Amino-1-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methoxypyrimidin-2-one | 37805-90-6 | C10H15N3O6 |
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—— | 2'-Chlor-2'-desoxy-Ψ-uridin | 4753-04-2 | C9H11ClN2O5 |
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—— | (S)-methyl-N-(1-phenylethyl)-2-azabicyclo[2.2.1]hept-5-ene-3-carboxylate | 130194-96-6 | C16H19NO2 |
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—— | 4-[(R)-[(2S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol | 524-63-0 | C19H22N2O2 |
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—— | (3R,6R)-6-[(1R,3aS,7aR)-4-[2-[(5S)-5-hydroxy-2-methylenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]-2-methylheptane-2,3-diol | 55721-11-4 | C27H44O3 |
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—— | 4-[(S)-[(2R,4R,5S)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol | 524-63-0 | C19H22N2O2 |
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—— | (4-bromo-2-fluorophenyl)(3,4,5-trimethoxyphenyl)methanone | 1016544-26-5 | C16H14BrFO4 |
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—— | (S)-6-(tert-butoxycarbonyl)-6-azaspiro[2.5]octane-5-carboxylic acid | 1262396-32-6 | C13H21NO4 |
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—— | dimethyl diazomethylphosphonate | 27491-70-9 | C3H8N2O3P |
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—— | N-(tert-butoxycarbonyl)-3-(1-(R)-α-naphthylethyl)-aminopyrrolidine | 870859-04-4 | C21H28N2O2 |
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—— | Phytonadione epoxide, (E,2S,3R)- | 25486-55-9 | C31H46O3 |
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—— | (R)-2-cyclopropyl-2-hydroxyacetic acid | 134624-47-8 | C5H8O3 |
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—— | 1'-([5-(aminomethyl)-1-(4,4,4-trifluorobutyl)-1H-1,3-benzodiazol-2-yl]methyl)-6'-fluoro-1',2'-dihydrospiro[cyclopropane-1,3'-indole]-2'-one | 1903763-82-5 | C23H22F4N4O |
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—— | 7-tert-butyl 6-hydrogen (1R,5S,6S)-3,3-dimethyl-2,4-dioxa-7-azabicyclo<3.3.0>octane-6,7-dicarboxylate | 127910-62-7 | C13H21NO6 |
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—— | 2,6-bis(3-isopropylphenyl)benzaldehyde | 934334-00-6 | C25H26O |
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—— | 1-(6-bromo-pyridin-2-yl)-3-carboethoxy-thiourea | 1010120-59-8 | C9H10BrN3O2S |
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—— | 5-tert-butylbenzo<b>thiophene-2-carboxylic acid | 126231-21-8 | C13H14O2S |
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—— | vimseltinib | 1628606-05-2 | C23H25N7O2 |
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—— | Cholesterylsulfat | 1256-86-6 | C27H46O4S |
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—— | 2-[Carbamoyl-[(5-nitrofuran-2-yl)methylideneamino]amino]acetic acid | 63981-22-6 | C8H8N4O6 |
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—— | 1-(2,4-dihydroxyphenyl)-3-(4-methylphenyl) propenone | 36574-88-6 | C16H14O3 |
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—— | cis-(3H,9aH)-3-Ethoxycarbonyl-chinolizidin | 19728-77-9 | C12H21NO2 |
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—— | (+/-)-(9a<i>r</i>)-octahydro-quinolizin-3<i>c</i>-carboxylic acid ethyl ester | 19728-76-8 | C12H21NO2 |
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—— | (2S,5R)-7-oxo-N-[(4R)-azepan-4-yl]-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide | 1174019-01-2 | C13H22N4O6S |
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