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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5-[(4-氨基苯甲酰)氨基]水杨酸 | 5-(4-amino-benzoylamino)-2-hydroxy-benzoic acid | 6201-78-1 | C14H12N2O4 |
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5-N,N-二乙基氨基-2-苯基磺酰基-2,4-戊二酸辛酯 | Octyl 5-N,N-diethylamino-2-phenylsulfonyl-2,4-pentadienoate | 98835-90-6 | C23H35NO4S |
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5-(羟甲基)吡唑-3-甲酸乙酯 | ethyl 3-(hydroxymethyl)-1H-pyrazole-5-carboxylate | 61453-48-3 | C7H10N2O3 |
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5-(溴甲基)-4-(4-氟苯基)-6-异丙基-2-[甲基(甲磺酰)氨基]嘧啶 | N-(5-(bromomethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide | 799842-07-2 | C16H19BrFN3O2S |
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5-(氯甲基)异邻苯二甲酸二甲酯 | dimethyl 5-(chloromethyl)isophthalate | 252210-01-8 | C11H11ClO4 |
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5-(氨基甲基)吲哚 | 5-aminomethylindole | 81881-74-5 | C9H10N2 |
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5-(戊烷-3-基氧基)-7-氧代-双环[4.1.0]庚-3-烯-3-羧酸乙酯 | ethyl (3R,4S,5S)-4,5-epoxy-3-(1-ethylpropoxy)-cyclohex-1-ene-1-carboxylate | 204254-96-6 | C14H22O4 |
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5-(哌嗪-1-基)苯并呋喃-2-甲酰胺 | 5-(1-piperazinyl)benzofuran-2-carboxamide | 183288-46-2 | C13H15N3O2 |
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5-(二氟甲氧基)-2-{[(4-氯-3-甲氧基-2-吡啶基)甲基]硫}-1氢-苯并咪唑 | 2-[(4-chloro-3-methoxy-2-pyridinyl)-methylthio]-5-difluoromethoxy-1H-benzimidazole | 368890-20-4 | C15H12ClF2N3O2S |
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5-(二氟甲基)-2-氨基-1,3,4-噻二唑 | 5-(difluoromethyl)-1,3,4-thiadiazol-2-amine | 25306-15-4 | C3H3F2N3S |
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5-(乙酰氨基)-N,N'-双(2,3-二羟基丙基)-2,4,6-三碘-1,3-苯二甲酰胺 | N,N'-bis(2,3-dihydroxypropyl)-5-acetamido-2,4,6-triiodoisophthalamide | 31127-80-7 | C16H20I3N3O7 |
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5-(三氟甲基)-1H-吡唑-3-胺 | 3-(trifluoromethyl)-1H-pyrazol-5-amine | 852443-61-9 | C4H4F3N3 |
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5-(4-羟基亚苄基)巴比妥酸 | 5-(4-hydroxybenzylidene)barbituric acid | 27406-31-1 | C11H8N2O4 |
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5-(4-甲氧基苯基)-1H-吡唑-3-羧酸 | 3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylic acid | 27069-16-5 | C11H10N2O3 |
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5-(2-溴乙基)-2,3-二氢苯并呋喃 | 2,3-dihydro-5-(2-bromoethyl)benzofuran | 127264-14-6 | C10H11BrO |
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5-(2-氯乙基)-2,3-二氢苯并呋喃 | 2-(2,3-dihydrobenzofuran-5-yl)ethylchloride | 943034-50-2 | C10H11ClO |
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5-(2-氟苯基)-N-甲基-1-(3-吡啶基磺酰基)-1H-吡咯-3-甲胺富马酸盐 | vonoprazan fumarate | 881681-01-2 | C4H4O4*C17H16FN3O2S |
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5-(2-氟-3-甲氧基苯基)-1-[[2-氟-6-(三氟甲基)苯基]甲基]-6-甲基-2,4(1H,3H)-嘧啶二酮 | 5-(2-fluoro-3-methoxyphenyl)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methylpyrimidine-2,4(1H,3H)-dione | 1150560-59-0 | C20H15F5N2O3 |
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5-(1H-吡咯烷-1-基)-2-巯基苯并咪唑 | 5-(1H-pyrrol-1-yl)-2-mercaptobenzimidazole | 172152-53-3 | C11H9N3S |
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5,8-二甲氧基-3,4-二氢-1H-2-萘酮 | 5,8-dimethoxy-2-tetralone | 37464-90-7 | C12H14O3 |
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5,8,11-十二烯酸 | 5,8,11-eicosatriynoic acid | 13488-22-7 | C20H28O2 |
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5,8,11,14,17,20-六氧杂-2-氮杂二十三碳二酸 1-(9H-芴-9-基甲基)酯 | fmoc-21-amino-4,7,10,13,16,19-hexaoxaheneicosanoic acid | 882847-34-9 | C30H41NO10 |
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5,7-二氢-7,7-二甲基-茚并[2,1-b]咔唑 | 5,7-dihydro-7,7-dimethylindeno[2,1-b]carbazole | 1257220-47-5 | C21H17N |
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5,6-反式-曲伏前列素 | [1R-[1α(E),2β(1E,3R*),3α,5α]]-7-[3,5-dihydroxy-2-[3-hydroxy-4-[3-(trifluoromethyl)phenoxy]-1-butenyl]cyclopentyl]-5-heptenoic acid 1-methylethyl ester | 1563176-59-9 | C26H35F3O6 |
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5,6-二甲基苯并咪唑 | 5,6-dimethyl-1H-benzo[d]imida-zole | 582-60-5 | C9H10N2 |
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5,6-二氢-3-(4-吗啉基)-1-(4-硝基苯基)-2(1H)-吡啶酮 | 3-morpholino-1-(4-nitrophenyl)-5,6-dihydropyridin-2(1H)-one | 503615-03-0 | C15H17N3O4 |
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5,6-二乙基-2,3-二氢-1H-茚-2-胺盐酸盐 | 5,6-diethyl-2,3-dihydro-1H-inden-2-amine hydrochloride | 312753-53-0 | C13H19N*ClH |
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5,6-二((4-甲氧基苄基)氧基)异苯并呋喃-1,3-二酮 | 5,6-bis((4-methoxybenzyl)oxy)isobenzofuran-1,3-dione | 1609071-04-6 | C24H20O7 |
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5,6,7,8-四氢-1,7-萘啶-3-羧酸乙酯盐酸盐 | ethyl 5,6,7,8-tetrahydro-1,7-naphthyridine-3-carboxylate hydrogen chloride | 1207175-08-3 | C11H14N2O2*ClH |
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5,5'-[1,1'-联苯]-4,4'-二基双[2-(2S)-2-吡咯烷基-1H-咪唑]四盐酸盐 | 4,4'-Bis(2-((S)-pyrrolidin-2-yl)-1H-imidazol-5-yl)-1,1'-biphenyl tetrahydrochloride | 1009119-83-8 | C26H32Cl4N6 |
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5,25R-胆甾烯-3beta,26-二醇 | (25R)-cholest-5-ene-3β,26-diol | 20380-11-4 | C27H46O2 |
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5,12-双(苯乙炔基)并四苯 | 5,12-Bis(phenylethynyl)naphthacene | 18826-29-4 | C34H20 |
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5,11-二氢-11-氯乙酰基-6H-吡啶并[2.3-b][1,4]苯并二氮卓-6-酮 | 11-(chloroacetyl)-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one | 28797-48-0 | C14H10ClN3O2 |
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5'-O-(二甲氧基三苯甲基)-N-异丁酰基-2'-脱氧胞苷 | N<sup>2</sup>-isobutyryl-5'-O-(4,4'-dimethoxytriphenylmethyl)-2'-deoxycytidine | 100898-62-2 | C34H37N3O7 |
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5'-O-(4,4'-二甲氧基三苯甲基)-N2-异丁酰基-2'-脱氧鸟苷-3'-(甲基-N,N-二异丙基)亚磷酰胺 | [(2R,3R,5R)-5-(2-Amino-6-oxo-3,6-dihydro-9H-purin-9-yl)-3-hydroxy-4,4-dimethoxy-5-(triphenylmethyl)oxolan-2-yl]methyl hydrogen phosphoramidoite | 84416-84-2 | C31H33N6O7P |
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4’-氯-2-硝基二苯醚 | 1-(4-chlorophenoxy)-2-nitrobenzene | 39145-47-6 | C12H8ClNO3 |
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4’-去甲基表鬼臼毒素-Β-D-葡萄糖甙 | 4'-demethyl-epipodophyllotoxin | 23363-35-1 | C27H30O13 |
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4’-(三氟甲基)联苯-4-甲醛 | 4-(4-trifluoromethylphenyl)benzaldehyde | 90035-34-0 | C14H9F3O |
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4-(甲基亚磺酰基)-苯乙酸 | 2-(4-(methylsulfinyl)phenyl)acetic acid | 118362-28-0 | C9H10O3S |
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4-(二甲氨基)-1,1-二甲氧基-3-丙烯-1-酮 | (E)-4-(dimethylamino)-1,1-dimethoxybut-3-en-2-one | 67751-23-9 | C8H15NO3 |
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4-酮13-顺式维甲酸 | 13-cis-4-Oxoretinoic acid | 71748-58-8 | C20H26O3 |
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4-苯氧基苄胺 | 4-phenoxybenzylamine | 107622-80-0 | C13H13NO |
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4-苯基-1-丁基溴 | 1-Bromo-4-phenylbutane | 13633-25-5 | C10H13Br |
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4-苄氧基-3-甲氧基苯乙酮 | 4-benzyloxy-3-methoxyacetophenone | 1835-11-6 | C16H16O3 |
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4-苄氧基-2-羟基苯乙酮 | 1-[4-(benzyloxy)-2-hydroxyphenyl]ethanone | 29682-12-0 | C15H14O3 |
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4-胺甲基苯甲醇 | 4-hydroxymethyl-benzylamine | 39895-56-2 | C8H11NO |
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4-肼基-N-甲基苯甲烷磺酰胺盐酸盐 | 4-hydrazino-N-methylbenzenemethanesulfonamide hydrochloride | 88933-16-8 | C8H13N3O2S*ClH |
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4-肼基-N-甲基苯甲烷磺胺 | N-[(4-Hydrazinophenyl)methyl]methanesulphonamide, hydrochloride | 81880-96-8 | C8H13N3O2S*ClH |
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4-羧基异噻唑 | isothiazole-4-carboxylic acid | 822-82-2 | C4H3NO2S |
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4-羟甲基苯甲酸 | 3-hydroxymethyl-benzoic acid | 3006-96-0 | C8H8O3 |
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