Sacubitril intermediate as well as preparation method and application thereof

The invention discloses a sacubitril intermediate as well as a preparation method and application thereof, relates to a medical intermediate, and can be used for efficiently preparing a key intermediate N-Boc amino alcohol [formula (10) or formula (10-a)]. The intermediates are useful in neutral end...

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Bibliographic Details
Main Authors ZHANG ZIHENG, ZHAO JINHUI, DING XIAOBING, LANG QIWEI, LIU CHUANGJI
Format Patent
LanguageChinese
English
Published 30.08.2022
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention discloses a sacubitril intermediate as well as a preparation method and application thereof, relates to a medical intermediate, and can be used for efficiently preparing a key intermediate N-Boc amino alcohol [formula (10) or formula (10-a)]. The intermediates are useful in neutral endopeptidase (NEP) inhibitors or prodrugs thereof, in particular, NEP inhibitors comprising a backbone of gamma-amino-delta-biphenyl-alpha-methyl alkanoic acid or ester, such as sacubitril and the like. The invention also provides an intermediate for preparing the compound (10) or the compound (10-a). The process route is cheap in raw materials, simple and convenient to operate, low in production cost and suitable for industrial production; 沙库必曲中间体、其制备方法及其应用，涉及医药中间体，本发明可以高效制备关键中间体N-Boc氨基醇[式(10)或式(10-a)]。所述的中间体可用于中性内肽酶(NEP)抑制剂或其前药，尤其地，包含γ-氨基-δ-联苯-α-甲基烷酸或酯的骨架的NEP抑制剂，如沙库必曲等。并且本发还提供了制备化合物(10)或化合物(10-a)的中间体。该工艺路线原料便宜、操作简便、生产成本低，适用于工业化生产，
Bibliography:Application Number: CN202210466737