[EN] PROCESS FOR PREPARING ALPHA AMINOACETALS IN RECEMIC FORM<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION D'ALPHA-AMINOACÉTALS SOUS FORME RACÉMIQUE
申请人:CLARIANT SPECIALTY FINE CHEM
公开号:WO2010031544A1
公开(公告)日:2010-03-25
The invention relates to a process for preparing an α-aminoacetal, or addition salts thereof, of formula (I) in recemic form comprising the steps consisting in: reacting a glyoxal monoacetal of formula (II) with an arylalkylamine of formula (III) in such a way as to obtain an imine of formula (IV); adding a Grignard reagent of formula R3-Mg-HaI to said imine of formula (IV) so as to obtain an amine of formula (V), and - deprotecting the amine of formula (V) in such a way as to obtain the compound of formula (I) in racemic form, and, where appropriate, adding an inorganic or organic acid in order to obtain an addition salt of the α-aminoacetal of formula (I).
This invention relates in general to certain substituted substituted 1,1,4-1l
6
-trioxo[1,2]thiazepan-4-ylamides of formula I
as defined herein which are protease inhibitors.