相似化合物
103322-56-1 58717-02-5 27527-05-5专利信息
专利号:US-5322963-A
优先权日:1991-02-05
标 题 :Method for preparing α-amino-β, δ-diol derivatives
发明人:SHIBATA SAIZO; SHIRAKAWA EIJI; YAMADA YASUKI; ANDO KOJI; UCHIDA ITSUO
权利人:JAPAN TOBACCO INC
摘要:Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of α-amino aldehyde derivative [I] and compound [II] in the presence of BF 3 .OEt 2 , as shown in the following reaction formula, α-amino-β-hydroxy-δ-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R 1 is a protective group on the amino group, R 2 is a lower alkyl group which may be branched, and R 4 is a cyclohexyl group or phenyl group).