PROCESS FOR PREPARING AZOLYL-PENTENE DERIVATIVES

摘要

Novel compds. (I) are prepd. by condensg. (CH3)2(RO)CC(=O) CH2R1 with R2C(=O)H. R=lower alkyl; R1=imidazol-1-yl or 1,2,4triazol-1-yl; R2=Ph, tienyl, furyl; Z=-CO- or -C(OH)H-. Dissolve 1-(2- chlorophenyl)-4-methoxy-4-methyl-2-(1,2,4-triazol-1-yl)-1pentene-3-on 10g (0.0327mol) in MeOH 25 ml, add NaBH4 0.57g (0.015 mole) at 0-10 deg.C with stirring for 15min, stir for 1hr and conc. by vacuum evaporator, add acetic acid, basify with K2CO3 soln., extract with ethyl acetate, dry on the MgSO4, conc. and recrystg. from diisopropyl ether to give 1-(2-chlorophenyl)-4methoxy-4-methyl-2-(1,2,4-triazol- 1-yl)-1-pentene-3-ol 5.2g (yield=51.7%, mp=116-118 deg.C).