| 摘要 |
PURPOSE:To effectively carry out cyclizaton reaction and obtain the titled compound useful as a raw material for medicines, by reacting a 2- halogenophenylalanine as a raw material in the coexistence of an amine and copper based catalyst. CONSTITUTION:A 2-halogenophenylalanine expressed by formula I [X is halogen; Y is OH, 1-10C (substituted) alkoxy, (substituted) aryloxy or amido residue], and ester or amide thereof is cylcized in the coexistence of an amine and copper based catalyst, e.g. anhydrous cupric chloride, preferably in an inert gas stream, e.g. N2, preferably at 100-200 deg.C for 2-8hr to afford the aimed compound expressed by formula II. Diethanolamine, tripropylamine, triethylamine, monoethanolamine, etc., may by used as the amine. USE:A raw material for producing (S)-1-[(S)-3-mercapto-2-oxopropyl]-indoline-2- carboxylic acid expressed by formula III, etc., useful as an angiotensin I converting enzyme inhibitor. |
