公开(公告)号：EP1595870A4

公开(公告)日：2009-02-25

申请号：EP04713193

申请日：2004-02-20

申请人： AJINOMOTO KK

发明人： KATAOKA NORIYASU ,  TATARA AKINORI ,  YATAGAI MASANOBU ,  YAMANAKA JUNKO

IPC分类号： C07C233/87 ,  C07D239/96 ,  C07C229/54 ,  C07C275/42

CPC分类号： C07D239/96 ,  C07C233/87

摘要： A process for producing a phenylalanine derivative which has a quinazolinedione ring and is represented by the formula (5), which comprises reacting an acylphenylalanine derivative represented by the formula (1) with a reagent for carbonyl group introduction and an anthranilic acid derivative to form an asymmetric urea intermediate, converting this asymmetric urea intermediate to a quinazolinedione compound in the presence of a base, and N-alkylating the resultant quinazolinedione compound at the amide group of the quinazolinedione ring with an N-alkylating agent. This process is suitable for the industrial production of the phenylalanine derivative containing a quinazolinedione skeleton, which is a compound highly useful as a medicine having integrin α4 inhibitory activity. In the formulae (1) and (5), R1 represents substituted phenyl, etc.; R2 represents alkyl, etc.; R3 represents dialkylamino, etc.; and R4 represents alkyl, etc.