PURPOSE: To obtain the subject azolysine useful as an intermediate for synthesis of medical and agricultural drugs.
CONSTITUTION: Compounds of formula I (R1 is lower alkyl; R2 is phenylalkyl or phenoxyalkyl phenyl ring hydrogen of which may be replaced with lower alkyl, halogen or lower alkoxy; R3 and R4 are lower alkyl; R5 is H; Z is O), e.g. 2-methyl-2-(3-p-chlorophenyl)propyl-4,4-dimethyloxazolysine. The above- mentioned compounds can be obtained by reacting a compound of formula II with a compound of formula III in the presence of a dehydration catalyst (e.g. p-toluenesulfonic acid) in a solvent (e.g. toluene) at 20-200°C for 0.3-24hr. The compound of formula III is used in an amount of 0.8-1.5 time mole based on the compound of formula II and the solvent is used so that the concentration of the compound of formula II may be 1-90wt.%. The catalyst is used in an amount of 0.001-0.1 time mole based on the compound of formula II.
NISHIMURA TAKASHI
YOKOYAMA SHUJI
