Method for preparing .alpha.-amino-.beta., .delta.-diol...

Details Method for preparing .alpha.-amino-.beta., .delta.-diol... Method for preparing .alpha.-amino-.beta., .delta.-diol...

C - Chemistry, Metallurgy

07

C

C07C 233/31 (2006.01) B01J 27/12 (2006.01) B01J 31/02 (2006.01) C07C 213/00 (2006.01) C07C 215/20 (2006.01) C07C 221/00 (2006.01) C07C 223/02 (2006.01) C07C 225/10 (2006.01) C07C 225/16 (2006.01) C07C 231/18 (2006.01) C07C 233/17 (2006.01) C07C 269/06 (2006.01) C07C 271/16 (2006.01) C07C 271/18 (2006.01)

Patent

CA 2079779

- 30 - A B S T R A C T Intermediate compounds (formula [III], [IV]) useful as starting material for amino acid derivatives which have renin inhibitory activity and are useful as remedies for hypertension are prepared stereoselectively at high yield, without requiring complicated process. In this method, by reaction of .alpha.-amino aldehyde deriva- tive [I] and compound [II] in the presence of BF3?OEt2, as shown in the following reaction formula, .alpha.-amino-.beta.- hydroxy-.delta.-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained. Image Image Image [I] [III] [IV] Image [II] (where R1 is a protective group of amino group, R2 is a lower alkyl group which may be branched, and R4 is a cyclohexyl group or phenyl group).

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