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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酒渣碱 | flazine | 100041-05-2 | C17H12N2O4 |
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邻苯二甲酸-1-丁酯-2-异丁酯 | butyl isobutyl phthalate | 17851-53-5 | C16H22O4 |
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邻乙基苯肼盐酸盐 | 2-ethylphenylhydrazine hydrochloride | 58711-02-7 | C8H12N2*ClH |
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邻三联苯 | o-terphenyl | 84-15-1 | C18H14 |
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达帕菲尼甲磺酸盐 | N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide methanesulfonate | 1195768-06-9 | CH4O3S*C23H20F3N5O2S2 |
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达帕菲尼中间体 | N-{3-[5-(2-chloro-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide | 1195768-23-0 | C23H18ClF3N4O2S2 |
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辣椒素酯 | capsiate | 205687-01-0 | C18H26O4 |
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辛波莫德半富马酸盐 | Siponimod fumarate | 1234627-85-0 | C62H74F6N4O10 |
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辛波莫德中间体 | 1-cyclohexyl-4-methyl-2-trifluoromethylbenzene | 1449293-48-4 | C14H17F3 |
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辛伐他汀杂质D | Simvastatin dimer | 476305-24-5 | C50H76O10 |
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贝美前列素中间体 | (5-(ethylamino)-5-oxopentyl)triphenylphosphonium bromide | 1201226-16-5 | Br*C25H29NOP |
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贝派地酸中间体 | 8-isocyano-2,2,14,14-tetramethyl-8-(toluene-4-sulfonyl)-pentadecanedioic acid diethyl ester | 738606-44-5 | C31H49NO6S |
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衣康酸盐 | 4-octyl itaconate | 3133-16-2 | C13H22O4 |
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螺[9H-芴-9,9'-[9H]呫吨]-3',6'-二醇 | spiro[fluorene-9,9'-xanthene]-3',6'-diol | 4081-00-9 | C25H16O3 |
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螺[3.5]壬烷-1,3-二酮 | 1-keto-3-hydroxy-spiro[3.5]non-2-ene | 455264-97-8 | C9H12O2 |
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螺[3.3]庚烷-2-羧酸 | spiro[3.3]heptane-2-carboxylic acid | 28114-87-6 | C8H12O2 |
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蓓萨罗丁中间体6 | methyl 4-<1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl>benzoate | 153559-48-9 | C25H30O2 |
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莱龙泰素中间体(A-3) | 7-deoxy-7β,8β-methanobaccatin III | 156294-33-6 | C31H36O10 |
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莫匹罗星锂 | Mupirocin lithium | 73346-79-9 | C26H43LiO9 |
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莠去津 | Atrazine-ring-UL-14C | 102029-43-6 | C8H14ClN5 |
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草酸二苄酯 | dibenzyl oxalate | 7579-36-4 | C16H14O4 |
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茶氨酸 | N-ethyl-L-glutamine | 3081-61-6 | C7H14N2O3 |
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茴茚二酮 | anisindione | 117-37-3 | C16H12O3 |
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茚满-5-磺酰氯 | indan-5-sulfonyl chloride | 52205-85-3 | C9H9ClO2S |
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苯磷硫胺 | benfotiamine | 22457-89-2 | C19H23N4O6PS |
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苯甲酸阿格列汀 | Alogliptin benzoate | 850649-62-6 | C7H6O2*C18H21N5O2 |
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苯甲酸,二氨基- | 2,3-diaminobenzoic acid | 603-81-6 | C7H8N2O2 |
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苯甲氧羰酰基四聚乙二醇羧乙基 | 3-oxo-1-phenyl-2,7,10,13,16-pentaoxa-4-azanonadecan-19-oic acid | 756526-00-8 | C19H29NO8 |
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苯甲孕酮 | 16α,17α-<(R)-1'-phenyl(ethylenedioxy)>pregn-4-ene-3,20-dione | 24356-94-3 | C29H36O4 |
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苯烯比妥 | 5-allyl-5-phenylbarbituric acid | 115-43-5 | C13H12N2O3 |
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苯并呋喃-4-甲酸 | benzofuran-4-carboxylic acid | 166599-84-4 | C9H6O3 |
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苯并二氢吡喃-8-硼酸 | chroman-8-ylboronic acid | 685514-79-8 | C9H11BO3 |
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苯并-1,4-二氧六环-6-硼酸 | 2.3-dihydro-1,4-benzodioxin-6-ylboronic acid | 164014-95-3 | C8H9BO4 |
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苯噻啶红地那非 | piperidinohongdenafil | 147676-50-4 | C24H31N5O3 |
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苯二酰亚氨乙醛二乙基乙缩醛 | phthalimidoacetaldehyde diethyl acetal | 78902-09-7 | C14H17NO4 |
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苯二甲酰亚氨基乙醛 | N-phthalimidyl-2-aminoacetaldehyde | 2913-97-5 | C10H7NO3 |
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苯丙酸,b-羟基-a-亚甲基-,甲基酯,(R)- | methyl (R)-3-hydroxy-3-phenyl-2-methylenepropanoate | 18020-59-2 | C11H12O3 |
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苯丙酸,b-羟基-a-亚甲基-,甲基酯,(R)- | methyl (S)-3-hydroxy-3-phenyl-2-methylenepropanoate | 18020-59-2 | C11H12O3 |
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苏型-(2RS)-4-苯基-3-乙酰氨基-2-羟基-4-氧代丁酸 | 2-benzyloxycarbonylsulfanyl-4,6-dimethyl-pyrimidine | 42116-21-2 | C14H14N2O2S |
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苄基辛基己二酸酯 | Benzyl octyl adipate | 3089-55-2 | C21H32O4 |
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苄基溴-d7 | perdeuteriobenzyl bromide | 35656-93-0 | C7H7Br |
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苄基异丁基甲醇 | 4-methyl-1-phenylpentan-2-ol | 7779-78-4 | C12H18O |
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芴甲氧羰基-L-缬氨酰-L-丙氨酸 | N-(9-fluorenylmethoxycarbonyl)-L-valyl-L-alanine | 150114-97-9 | C23H26N2O5 |
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芴丁酯 | 9-hydroxy-9-fluorene carboxylic acid | 467-69-6 | C14H10O3 |
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芬地柞酸 | 2-<(2'-hydroxy-5'-biphenylyl)carbonyl>benzoic acid | 84627-04-3 | C20H14O4 |
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艾瑞芬净 | ibrexafungerp | 1207753-03-4 | C44H67N5O4 |
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艾沙康唑中间体7 | (2S,3R)-3-(2,5-difluorophenyl)-3-hydroxy-2-methyl-4-(1H-1,2,4-triazol-1-yl)butanenitrile | 241479-74-3 | C13H12F2N4O |
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艾沙康唑中间体6 | (2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-2-methyl-4-(1H-1,2,4-triazol-1-yl)butanamide | 241479-75-4 | C13H14F2N4O2 |
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艾氟康唑中间体2 | 1-[(2R,3R)-2-(2,4-difluorophenyl)-2,3-dihydroxybutyl]-1H-[1,2,4]triazole methanesulfonate salt | 1175536-50-1 | CH4O3S*C12H13F2N3O2 |
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艾日布林中间体 | 3-((2S,5S)-5-(2-((2S,4R,6R)-6-(((2S,3S,4R,5R)-5-((S)-2,3-bis((tert-butyldimethylsilyl)oxy)propyl)-4-methoxy-3-((phenylsulfonyl)methyl)tetrahydrofuran-2-yl)methyl)-4-methyl-5-methylenetetrahydro-2H-pyran-2-yl)ethyl)-4-methylenetetrahydrofuran-2-yl)propan-1-ol | 253128-10-8 | C45H78O9SSi2 |
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