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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(S)-3,3-二甲基-2-((((1R,2R)-2-(戊-4-烯-1-基)环丙氧基)羰基)氨基)丁酸 | 3-methyl-N-({[(1R,2R)-2-pent-4-en-1-ylcyclopropyl]oxy}carbonyl)-L-valine | 1026200-27-0 | C15H25NO4 |
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(S)-3,10-二溴-6-苯基-6H-苯并[5,6][1,3]噁嗪并[3,4-a]吲哚 | (S)-3,10-dibromo-6-phenyl-6H-benzo[5,6][1,3]oxazino[3,4-a]indole | 1392102-38-3 | C21H13Br2NO |
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(S)-2-苄基-N,N-二甲基氮丙啶-1-磺酰胺 | (S)-2-benzyl-N,N-dimethylaziridine-1-sulfonamide | 902146-43-4 | C11H16N2O2S |
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(S)-2-苄基-3-((3r,4r)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基)丙酸甲酯盐酸盐 | (2S)-2-([(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl)-3-phenylpropanoic acid methyl ester hydrochloride | 170098-28-9 | C24H31NO3*ClH |
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(S)-2-溴-Alpha-甲基苯甲醇 | (1S)-1-(2-bromophenyl)ethanol | 114446-55-8 | C8H9BrO |
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(S)-2-氨基辛二酸 | L-2-aminosuberic acid | 4254-88-0 | C8H15NO4 |
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(S)-2-氨基-5-甲氧基四氢萘盐酸盐 | (S)-5-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine hydrochloride | 58349-17-0 | C11H15NO*ClH |
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(S)-2-氨基-4-甲基-1-((R)-2-甲基环氧乙烷-2-基)-1-戊酮三氟乙酸盐 | (2S)-2-amino-4-methyl-1-[(2R)-2-methyloxiranyl]-1-pentanone trifluoroacetate | 247068-85-5 | C2HF3O2*C9H17NO2 |
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(S)-2-氨基-2-(3-氟苯基)乙醇-1-醇盐酸盐 | (S)-2-amino-2-(3-fluorophenyl)ethanol hydrochloride | 1240480-36-7 | C8H10FNO*ClH |
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(S)-2-二甲基氨基-1-苯基乙醇 | (S)-2-dimethylamino-1-phenylethanol | 2202-68-8 | C10H15NO |
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(S)-2-乙基丁基2-氨基丙酸酯盐酸盐 | L-alanine 2-ethylbutyl ester hydrochloride | 946511-97-3 | C9H19NO2*ClH |
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(S)-2-(苄氧基)-1-(吡咯烷-1-基)丙烷-1-酮 | (S)-2-(benzyloxy)-1-(pyrrolidin-1-yl)propan-1-one | 122151-32-0 | C14H19NO2 |
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(S)-2-(丁-3-烯基)环氧乙烷 | (S)-1,2-epoxy-5-hexene | 137688-21-2 | C6H10O |
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(S)-2-(n-boc-氨基)-n-苄氧基-3-羟基-3-甲基丁酰胺 | (S)-tert-butyl 1-(benzyloxyamino)-3-hydroxy-3-methyl-1-oxobutan-2-ylcarbamate | 102507-19-7 | C17H26N2O5 |
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(S)-2-(3-吡咯烷)-2-丙醇盐酸盐 | (S)-2-(3-pyrrolidinyl)-2-propanol hydrochloride salt | 1272755-91-5 | C7H15NO*ClH |
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(S)-2-(((9H-芴-9-基)甲氧基)羰基)氨基)-3-(四氢-2H-吡喃-4-基)丙酸 | (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(tetrahydro-2H-pyran-4-yl)propanoic acid | 368866-34-6 | C23H25NO5 |
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(S)-2-((((9h-芴-9-基)甲氧基)羰基)氨基)-6-(((4-甲氧基苯基)二苯基甲基)氨基)己酸 | Fmoc-Lys(Mmt)-OH | 159857-60-0 | C41H40N2O5 |
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(S)-2-((((9H-芴-9-基)甲氧基)羰基)(甲基)氨基)-4-甲氧基-4-氧代丁酸 | Fmoc-N-Me-Asp(OMe)-OH | 2044710-58-7 | C21H21NO6 |
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(S)-2,5-二氢-1H-吡咯-2-羧酸 | tert-butyl (1R,5S)-3-amino-8-azabicyclo[3.2.1]octane-8-carboxylate | 744183-20-8 | C12H22N2O2 |
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(S)-2,4-二氯-A-甲基-苯甲胺盐酸盐 | 2,6-dichlorophenylethylamine | 133492-69-0 | C8H9Cl2N |
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(S)-1-苯基-1,2,3,4-四氢异喹啉 | (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline | 118864-75-8 | C15H15N |
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(S)-1-溴-3-(1-(己氧基)乙基)-2-甲氧基苯 | (S)-1-bromo-3-(1-hexyloxyethyl)-2-methyloxybenzene | 1110767-94-6 | C15H23BrO2 |
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(S)-1-氨基-3-氯-2-丙醇盐酸盐 | (S)-1-amino-3-chloro-2-propanol hydrochloride | 34839-13-9 | C3H8ClNO*ClH |
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(S)-1-氨基-2,3-二氢-1H-茚-4-腈盐酸盐 | (S)-1-amino-2,3-dihydro-1H-indene-4-carbonitrile hydrochloride | 1306763-57-4 | C10H10N2*ClH |
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(S)-1-对甲苯磺酰基-3-(1-氰基-1,1-二苯甲基)吡咯烷 | (S)-2,2-diphenyl-2-(1-tosyl-3-pyrrolidinyl)acetonitrile | 133099-09-9 | C25H24N2O2S |
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(S)-1-叔丁氧羰基-3-羟基哌啶 | tert-butyl (3S)-3-hydroxypiperidine-1-carboxylate | 143900-44-1 | C10H19NO3 |
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(S)-1-[3,5-二(三氟甲基)苯基]乙醇 | (S)-3,5-bis(trifluoromethyl)-1-phenylethanol | 225920-05-8 | C10H8F6O |
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(S)-1-Boc-吡咯烷-3-甲酸 | (S)-1-N-boc-β-proline | 140148-70-5 | C10H17NO4 |
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(S)-1-Boc-2-异丙基哌嗪 | (S)-tert-butyl 2-isopropylpiperazine-1-carboxylate | 674792-05-3 | C12H24N2O2 |
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(S)-1-(3-甲氧基苯基)乙胺盐酸盐 | (S)-1-(3-methoxyphenyl)ethylammonium chloride | 1304771-27-4 | C9H13NO*ClH |
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(S)-1-(2,6-二氯-3-氟苯基)乙醇 | (S)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol | 877397-65-4 | C8H7Cl2FO |
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(S)-(2,2-二甲基-1,3-二氧环戊烷-4-基)甲基 3-(4-羟基苯基)丙酸酯 | (S)-(2,2-dimethyl-1,3-dioxolan-4-yl)methyl 3-(4-hydroxyphenyl)propanoate | 144256-11-1 | C15H20O5 |
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(S)-(-)-alpha-(Boc-氨基)-gamma-丁酸内酯 | tert-butyl (3S)-2-oxotetrahydrofuran-3-ylcarbamate | 40856-59-5 | C9H15NO4 |
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(S)-(-)-4-羟基-2-吡咯烷酮 | (4S)-4-hydroxypyrrolidin-2-one | 68108-18-9 | C4H7NO2 |
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(S)-(-)-3-环己烯甲酸 | (1S)-3-cyclohexenecarboxylic acid | 5708-19-0 | C7H10O2 |
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(S)-(+)-N,N-二甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺草酸盐 | (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine oxalate | 132335-47-8 | C2H2O4*C19H21NOS |
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(S)-(+)-2,2-二甲基环丙烷甲酰胺 | (S)-2,2-dimethylcyclopropanecarboxamide | 75885-58-4 | C6H11NO |
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(S)-(+)-1,2-丙二醇 | (S)-1,2-Propanediol | 4254-15-3 | C3H8O2 |
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(R,S)-1-对甲苯磺酰基甘油 | (+/-)-2,3-dihydroxypropyl tosylate | 73073-07-1 | C10H14O5S |
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(R,R)-1,2-双(甲磺酰基氧基甲基)环己烷 | (1R,2R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane | 186204-35-3 | C10H20O6S2 |
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(R,E)-5-([1,1'-联苯]-4-基)-4-[(叔丁氧羰基)氨基]-2-甲基-2-戊烯酸 | (R,E)-5-([1,1'-biphenyl]-4-yl)-4-((tert-butoxycarbonyl)amino)-2-methyl-2-pentenoic acid | 1012341-48-8 | C23H27NO4 |
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(R)-色满-2-基甲胺盐酸盐 | (2R)-3,4-dihydro-2H-chromen-2-ylmethylamine hydrochloride | 437763-66-1 | C10H13NO*ClH |
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(R)-氟甲喹 | R-(+)-flumequine | 215178-95-3 | C14H12FNO3 |
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(R)-普瑞巴林 | (R)-pregabalin | 148553-51-9 | C8H17NO2 |
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(R)-四氢呋喃甲酸 | (R)-tetrahydro-2-furoic acid | 87392-05-0 | C5H8O3 |
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(R)-依法韦仑 | (R)-efavirenz | 154801-74-8 | C14H9ClF3NO2 |
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(R)-二氢-4-丙基-2(3H)-呋喃酮 | (R)-4-propyldihydrofuran-2(3H)-one | 63095-51-2 | C7H12O2 |
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(R)-β2-高缬氨酸 | (R)-2-(Aminomethyl)-3-methylbutanoic acid hydrochloride | 1276055-45-8 | C6H13NO2*ClH |
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(R)-N-Boc-2-羟甲基吗啉 | (R)-2-hydroxymethylmorpholine-4-carboxylic acid tert-butyl ester | 135065-71-3 | C10H19NO4 |
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(R)-N-(1-(3-(苄氧基)-2-羟基丙基)-2-(1-(苄氧基)-2-甲基丙-2-基)-6- | (R)-N-(1-(3-(benzyloxy)-2-hydroxypropyl)-2-(1-(benzyloxy)-2-methylpropan-2-yl)-6-fluoro-1H-indol-5-yl)-1-(2,2-difluorobenzo [d][1,3]dioxol-5-yl)cyclopropanecarboxamide | 1294504-68-9 | C40H39F3N2O6 |
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