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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6-(4-甲基哌嗪-1-基)-4-(2-甲基苯基)烟酰胺 | 4-(2-methylphenyl)-6-(4-methylpiperazinyl)-3-pyridinecarboxamide | 342417-01-0 | C18H22N4O |
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6-(4-氯苯基)-2-氧代-1,2-二氢-3-吡啶羧酸 | p-propoxyphenylacetic acid | 26118-57-0 | C11H14O3 |
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6-(4-氯苯基)-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯里嗪 | 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine | 133111-56-5 | C21H20ClN |
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6-(4-氨基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮 | 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3(2H)-pyridazinone | 36725-28-7 | C11H13N3O |
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6-(4-氨基苯基)-1-(4-甲氧基苯基)-7-氧代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-3-羧酸乙酯 | ethyl 6-(4-aminophenyl)-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate | 503615-07-4 | C22H22N4O4 |
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6-(2,6-二氯苯基)-2-[(4-氟-3-甲基苯基)氨基]-8-甲基吡啶并[2,3-d]嘧啶-7(8H)-酮 | 6-(2,6-Dichlorophenyl)-2-[(4-Fluoro-3-Methylphenyl)amino]-8-Methylpyrido[2,3-D]pyrimidin-7(8h)-One | 287204-45-9 | C21H15Cl2FN4O |
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6-(10-羟基癸酰基)-2,3-二甲氧基-5-甲酚 | 6-(10-hydroxy-1-oxodecyl)-2,3-dimethoxy-5-methylphenol | 104966-97-4 | C19H30O5 |
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6-(1-吡咯烷并)吡啶-3-硼酸频哪醇酯 | 2-(pyrrolidin-1-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine | 933986-97-1 | C15H23BN2O2 |
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6,9-二氟-11,17-二羟基-16-甲基-3-氧代雄甾-1,4-二烯-17-羧酸 | 6α,9α-difluoro-11β,17α-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carboxylic acid | 28416-82-2 | C21H26F2O5 |
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6,7-二羟基-4-(三氟甲基)香豆素 | 6,7-dihydroxy-4-trifluoromethyl-2H-chromen-2-one | 82747-36-2 | C10H5F3O4 |
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6,7-二甲氧基-4-(4-氨基苯氧基)喹啉 | 4-((6,7-dimethoxyquinolin-4-yl)oxy)aniline | 190728-25-7 | C17H16N2O3 |
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6,7-二甲氧基-1(S)-[2-[4-(三氟甲基)苯基]乙基]-1,2,3,4-四氢异喹啉 | (S)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-1,2,3,4-tetrahydroisoquinoline | 769172-81-8 | C20H22F3NO2 |
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6,7-二甲氧乙氧基喹唑啉-4-酮 | 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one | 179688-29-0 | C14H18N2O5 |
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6,7-二氢-2H-吡唑并[4,3-c]吡啶-5(4h)-羧酸叔丁酯 | tert-butyl 1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxylate | 924869-27-2 | C11H17N3O2 |
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6,6-二甲基二环[3.3.1]庚-2-烯-2-丙醛 | pinoacetaldehyde | 33885-51-7 | C12H18O |
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6,6-二甲基-3-氮杂双环[3.1.0]己烷-2,4-二酮 | 6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2,4-dione | 194421-56-2 | C7H9NO2 |
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6,6-二甲基-3-氮杂双环[3.1.0]己烷 | 6,6-dimethyl-3-azabicyclo[3.1.0]hexane | 943516-54-9 | C7H13N |
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6,11-二氢-11-氧代二苯并[b,e]氧杂卓-2-乙酸甲酯 | isoxepac methyl ester | 55689-64-0 | C17H14O4 |
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6(or7)-氨基-2-萘磺酸 | Bronner acid | 93-00-5 | C10H9NO3S |
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5alpha-雄甾-2-烯-17-酮 | 5α-androst-2-en-17-one | 963-75-7 | C19H28O |
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5alpha-孕甾-3alpha-醇-20-酮 | tetrahydroprogesterone | 516-54-1 | C21H34O2 |
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5H-[1]苯并噻吩并[3,2-C]咔唑 | 5H-benzo[4,5]thieno[3,2-c]carbazole | 1255308-97-4 | C18H11NS |
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5A-羟基拉肖皂苷元 | (25R)-3β,5α-dihydroxy-spirostan-6-one | 56786-63-1 | C27H42O5 |
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525-氨基-2-(26-二氧代哌啶-3-基)异二氢吲哚-13-二酮 | 5-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione | 191732-76-0 | C13H11N3O4 |
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5-香叶氧基-7-甲氧基香豆素 | 5-geranyloxy-7-methoxycoumarin | 7380-39-4 | C20H24O4 |
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5-降冰片烯-2-羧酸甲酯 | methyl 5-norbornene-2-carboxylate | 6203-08-3 | C9H12O2 |
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5-苯氧基-3-吡啶基)硼酸 | 5-phenoxy-3-pyridinylboronic acid | 850991-33-2 | C11H10BNO3 |
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5-苯基-2,3,7-三(苯基氨基)吩嗪鎓氯化物 | 2,3,7-trianilino-5-phenyl-phenazinium; chloride | 4935-81-3 | C36H28N5*Cl |
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5-苯基-2,3,7,8-四(苯基氨基)吩嗪鎓氯化物 | 2,3,7,8-tetraanilino-5-phenyl-phenazinium; chloride | 4935-82-4 | C42H33N6*Cl |
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5-苄硫基四氮唑 | 5-(benzylthio)-1H-tetrazole | 21871-47-6 | C8H8N4S |
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5-苄烯海因 | 5-benzylidenehydantoin | 3775-01-7 | C10H8N2O2 |
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5-羟甲基尿苷 | 5-(hydroxymethyl)uridine | 30414-00-7 | C10H14N2O7 |
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5-羟甲基噻唑 | thiazol-5-yl-methanol | 38585-74-9 | C4H5NOS |
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5-羟基吲哚 | indol-5-ol | 1953-54-4 | C8H7NO |
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5-羟基-4-甲氧基-2-硝基苯甲醛 | 3-hydroxy-4-methoxy-6-nitrobenzaldehyde | 58749-47-6 | C8H7NO5 |
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5-羟基-3,4-二氢-2-喹啉酮 | 5-hydroxycarbostyril | 30389-33-4 | C9H9NO2 |
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5-碘吲哚 | 5-iodo-1H-indole | 16066-91-4 | C8H6IN |
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5-硼酸频那醇酯吲哚-2-酮 | 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolin-2-one | 837392-64-0 | C14H18BNO3 |
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5-硝基荧光素 | 4'-nitrofluorescein | 27402-68-2 | C20H11NO7 |
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5-硝基-Α-四氢萘酮 | 5-nitro-1-tetralone | 51114-73-9 | C10H9NO3 |
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5-硝基-2-茚酮 | 5-nitro-2-indanone | 116530-60-0 | C9H7NO3 |
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5-甲苯磺酰基-5H-吡咯并[2,3-B]吡嗪-2-胺基甲酸叔丁酯 | tert-butyl (5-tosyl-5H-pyrrolo[2,3-b]pyrazin-2-yl)carbamate | 1201187-44-1 | C18H20N4O4S |
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5-甲氧基色胺盐酸盐 | 5-methoxytryptamine hydrochloride | 17107-33-4 | C11H14N2O*ClH |
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5-甲氧基胞苷 | 5-methoxycytidine | 37805-90-6 | C10H15N3O6 |
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5-甲氧基-6-硝基吡啶甲酸甲酯 | 5-methoxy-6-nitro-pyridine-2-carboxylic acid methyl ester | 390816-44-1 | C8H8N2O5 |
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5-甲氧基-1,2,3,4-四氢-N-(苯甲基)-2-萘胺 | 2-(N-benzylamino)-5-methoxytetralin | 136247-07-9 | C18H21NO |
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5-甲基色胺盐酸盐 | 5-methyltryptamine hydrochloride | 1010-95-3 | C11H14N2*ClH |
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5-甲基异恶唑-4-甲酸 | 5-methyl-1,2-oxazole-4-carboxylic acid | 42831-50-5 | C5H5NO3 |
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5-甲基吲哚-3-甲酸甲酯 | methyl 5-methyl-1H-indole-3-carboxylate | 227960-12-5 | C11H11NO2 |
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5-甲基吡嗪-2-羧酸 | 2-methylpyrazin-5-carboxylic acid | 5521-55-1 | C6H6N2O2 |
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