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【结 构 式】

【分子编号】62824

【品名】D-norvaline

【CA登记号】

【 分 子 式 】C5H11NO2

【 分 子 量 】117.14788

【元素组成】C 51.26% H 9.46% N 11.96% O 27.31%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(IX)

Diazotization of (R)-2-aminopentanoic acid (IX) in the presence of HBr/KBr gives rise to the configuration-retained alpha-bromoacid (X). This is further coupled to the dipeptide ester (VIII) in the presence of EDC/HOAt to furnish the corresponding alpha-bromo amide (XI). Finally, displacement of the bromide group of (XI) with potassium thioacetate in DMF leads to the target thioacetate ester.

1 Fink, C.A.; De Lombaert, S.; Hoyer, D.W.; Jeng, A.Y.; Firoozina, F. (Novartis AG; Novartis Pharma GmbH); Certain thiol inhibitors of endothelin-converting enzyme. WO 9955726 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(VIII) 62823 methyl (2S)-2-{[(1-aminocyclopentyl)carbonyl]amino}-3-[1,1'-biphenyl]-4-ylpropanoate C22H26N2O3 详情 详情
(IX) 62824 D-norvaline C5H11NO2 详情 详情
(X) 62825 (2R)-2-bromopentanoic acid C5H9BrO2 详情 详情
(XI) 62826 methyl (2S)-3-[1,1'-biphenyl]-4-yl-2-{[(1-{[(2R)-2-bromopentanoyl]amino}cyclopentyl)carbonyl]amino}propanoate C27H33BrN2O4 详情 详情
Extended Information