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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奥泽沙星中间体E | 7-{6-[benzoyl(methyl)amino]-5-methyl-3-pyridinyl}-1-cyclopropyl-8-methyl-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid ethyl ester | 446299-90-7 | C30H29N3O4 |
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奥泽沙星中间体B | (5-bromo-6-methylpyridin-2-yl)methylamine | 245765-66-6 | C7H9BrN2 |
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奥泽沙星中间体 | ethyl 1-cyclopropyl-8-methyl-7-chloro-4-oxo-1,4-dihydroquinolin-3-carboxylate | 103877-51-6 | C16H16ClNO3 |
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奥沙特隆 | 2-oxachlormadinone | 105149-04-0 | C20H25ClO4 |
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奥扎莫德盐酸盐 | ozanimod hydrochloride | 1618636-37-5 | C23H24N4O3*ClH |
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奥利司他杂质 | Orlistat open ring epimer | 130793-28-1 | C29H55NO6 |
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奎尼卡因 | Dimethisoquin | 86-80-6 | C17H24N2O |
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奎宁环 | Quinuclidine | 100-76-5 | C7H13N |
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头孢维欣 | Cefovecin | 234096-34-5 | C17H19N5O6S2 |
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头孢甲肟杂质13 | (6<i>R</i>)-7<i>t</i>-amino-3-(1-methyl-1<i>H</i>-tetrazol-5-ylsulfanylmethyl)-8-oxo-(6<i>r</i><i>H</i>)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid | 24209-38-9 | C10H12N6O3S2 |
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头孢洛仑 | cephaloram | 859-07-4 | C18H18N2O6S |
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头孢替考 | Cefetecol | 117211-03-7 | C20H17N5O9S2 |
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头孢妥仑酯的中间体 | p-Methoxybenzyl 7-phenylacetamido-3(Z)-(4-methylthiazol-5-yl)vinyl-3-cephem-4-carboxylate | 138514-31-5 | C29H27N3O5S2 |
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头孢地尼异恶唑 | (6R,7R)-7-(4-Hydroxyisoxazole-3-carboxamido)-8-oxo-3-vinyl-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid | 1356842-10-8 | C13H11N3O6S |
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头孢地尔 | cefiderocol | 1225208-94-5 | C30H34ClN7O10S2 |
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头孢卡奈 | Cefcanel | 41952-52-7 | C19H18N4O5S3 |
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头孢三唑 | Cefetrizole | 65307-12-2 | C16H15N5O4S3 |
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多西他赛缩合物中间体 | 5-O-[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-2-benzoyloxy-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-9,12-bis(2,2,2-trichloroethoxycarbonyloxy)-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-15-yl] 3-O-tert-butyl (4S,5R)-2-(4-methoxyphenyl)-4-phenyl-1,3-oxazolidine-3,5-dicarboxylate | 859498-31-0 | C57H61Cl6NO19 |
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外消旋鲁替替尼-d8 | ruxolitinib | 941688-05-7 | C17H18N6 |
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外消旋5,6-去氢普瑞巴林 | 3-(aminomethyl)-5-methylhex-5-enoic acid | 1136478-30-2 | C8H15NO2 |
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外向-8-苄基-8-氮杂双环[3.2.1]辛-3-胺 | 8-benzyl-8-azabicyclo[3.2.1]octan-3-amine | 76272-36-1 | C14H20N2 |
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塞拉非莫德 | 1-({6-[(2-methoxy-4-propylbenzyl)oxy]-1-methyl-3,4-dihydronaphthalen-2-yl}methyl)azetidine-3-carboxylic acid | 891859-12-4 | C27H33NO4 |
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塞尔帕替尼 | 4-(5-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyrazin-2-yl)-6-(((R)-morpholin-2-yl)methoxy)pyrazolo[1,5-a]pyridine-3-carbonitrile | 2222755-14-6 | C29H31N9O3 |
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培磷酰胺 | 4-hydroperoxycyclophosphamide | 39800-16-3 | C7H15Cl2N2O4P |
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地麦威 | 5,5-dimethyl-3-oxocyclohex-1-en-1-yl dimethylcarbamate | 122-15-6 | C11H17NO3 |
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地美环素 | demeclocycline | 127-33-3 | C21H21ClN2O8 |
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地瑞那韦中间体1 | 1-[[[(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yloxy]carbonyl]oxy]pyrrolidine-2,5-dione | 253265-97-3 | C11H13NO7 |
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地瑞拉韦中间体2 | tert-butyl N-[(2S,3R)-4-[benzyl(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate | 1213710-57-6 | C26H38N2O3 |
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地屈孕酮二(乙烯缩醛) | 9β,10α-dehydroprogesterone diethylene ketal | 5488-51-7 | C25H36O4 |
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地塞米松环氧水解物 | 17α,21-dihydroxy-9β,11β-oxido-16α-methylpregna-1,4-diene-3,20-dione | 24916-90-3 | C22H28O5 |
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地塞米松-17-酮(非对映异构体混合物) | (9R,10S,11S,13S,16S)-9-fluoro-11-hydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione | 1880-61-1 | C20H25FO3 |
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图卡替尼N-4 | 7-(2-methyl-4-nitrophenoxy)-[1,2,4]triazolo[1,5-a]pyridine | 937263-44-0 | C13H10N4O3 |
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图卡替尼N-1 | 1-(4-((4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)quinazolin-6-yl)-3-(1-hydroxy-2-methylpropan-2-yl)thiourea | 1429755-58-7 | C26H26N8O2S |
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四苯基氯化膦 | tetraphenyl phosphonium chloride | 2001-45-8 | C24H20P*Cl |
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四甲基久洛尼定 | 1,1,7,7-tetramethyl-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-8-ol | 115704-83-1 | C16H23NO |
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四烯孕二酮 | pregna-1,4,9(11),16(17)-tetraene-3,20-dione | 117048-56-3 | C21H24O2 |
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四溴苯酐二钠 | Disodium tetrabromophthalate | 25357-79-3 | C8Br4Na2O4 |
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四氮唑乙酸 | 1H-tetrazol-1-ylacetic acid | 21732-17-2 | C3H4N4O2 |
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四氢呋喃-2-甲醛 | tetrahydrofuran-2-carbaldehyde | 7681-84-7 | C5H8O2 |
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四(十八烷基)高氯酸铵 | Tetraoctadecylammonium perchlorate | 139653-59-1 | C72H148ClNO4 |
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噻奈普汀乙酯 | ethyl 7-((3-chloro-6-methyl-5,5-dioxido-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-yl)amino)heptanoate | 66981-77-9 | C23H29ClN2O4S |
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噻唑-5-甲酸乙酯 | ethyl thiazole-5-carboxylate | 32955-22-9 | C6H7NO2S |
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噻吩-3-基-乙酰氯 | 2-(thiophen-3-yl)acetyl chloride | 13781-65-2 | C6H5ClOS |
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噻吩-2,3-二甲醛 | 2,3-diformylthiophene | 932-41-2 | C6H4O2S |
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噻前列素 | 7-[3,5-dihydroxy-2-(3-hydroxy-4-thiophen-3-yloxybut-1-enyl)cyclopentyl]hept-5-enoic acid | 71116-82-0 | C20H28O6S |
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喹唑啉-6-羧酸 | quinazoline-6-carboxylic acid | 676326-53-7 | C9H6N2O2 |
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哒螨酮,1-氨基-碘(1∶1) | pyridazin-1-ium-1-amine iodide | 35073-04-2 | C4H6N3*I |
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哌嗪-N,N’-二(2-羟基丙磺酸)倍半钠盐 | POPSO sesquisodium salt | 108321-08-0 | C20H41N4Na3O16S4 |
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哌啶-4-基-乙酸叔丁基酯 | tert-butyl 2-(piperidin-4-yl)acetate | 180182-07-4 | C11H21NO2 |
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哈敏1622 | methyl benzethonium chloride | 25155-18-4 | C28H44NO2*Cl |
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