公开(公告)号：EP1451147A4

公开(公告)日：2007-06-06

申请号：EP02752525

申请日：2002-07-24

申请人： PHARMACORE INC

发明人： ALLA SEKAR ,  CHOI SEUNG-YONG ,  ZHANG WEN-CHUN ,  DHANOA DALE ,  DIFRANCO ELSO ,  KROKHINA GALINA ,  LI KEQIANG ,  THIAGARAJAN BALASUBRAMANIAN

IPC分类号： C07C229/28 ,  C07C229/36 ,  C07C271/22 ,  C07D211/34 ,  C07D213/55 ,  C07D309/04 ,  C07D333/24 ,  C07D335/02

CPC分类号： C07C229/36 ,  C07C229/28 ,  C07C271/22 ,  C07C2602/18 ,  C07C2603/18 ,  C07D211/34 ,  C07D213/55 ,  C07D309/04 ,  C07D333/24 ,  C07D335/02

摘要： The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. The present invention also provides a novel method for the synthesis of alpha-amino acids and derivatives thereof. The alpha-amino acids and derivatives thereof may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate, and a C1-C6 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.