| 摘要 |
A process for preparing 1-acyl-pyrrolidine-2-carbonitrile derivs. of formula (I) comprises (A) reaction of (II) with 2chloroacrylonitrile, sodium borohydride or potassium borohydride to form (III) and (B) cyclization of (III) by reacting with base in a non-protonic solvent opt. adding a phase-converting catalyst. In the formulas, R1 and R2 each= C1-6 alkyl or C6-10 aryl or together represent -(CH2)N- or - (CH2)P-CH=CH-(CH2)Q wherein n= 3-6, p+q= 1-4; R3= C1-5 alkyl or C6-10 aryl, pref. phenyl; X= halogen, pseudohalogen or acetate. (I) are useful as intermediates for proline cpds. with angiotensin converting enzyme inhibiting activity.
|
