| 摘要 |
<p>PURPOSE:To produce an optically active beta-amino acid which is useful as a synthetic intermediate for physiologically active peptides and an important intermediate for beta-lactam antibiotics in high optical purity. CONSTITUTION:(Z)-3-N-acylamino-3-substituted-alkylacrylic ac id of formula I (R<1> is lower alkyl, phenyl, benzyloxy; R<2> is lower alkyl where its hydrogen atoms may be substituted with phenyl or alkoxycarbonyl). For example, (Z)-3-N- benzamide-2-hexenoic acid is asymmetrically hydrogenated using an optically active Ru-phosphine complex as a catalyst to give an optically active 3-N- acylamino-3-substituted alkylpropionic acid of formula II such as (3S)-(+)-3- benzamidehexanoic acid. Further the compound of formula II is subjected to deacylation into an optically active beta-amino acid. As a catalyst described above, is cited a compound of formula IV or V [R<4>-BTNAP is formula VI (R<4> is H, lower alkyl); Y is BF<-4>, PF<-6>, ClO4<->, SbF<-6>].</p> |
