| 摘要 |
A process for prepg. 3-(2-guanidino-4-thiazolylmethylthio) propion nitrile of formula (I) comprises (a) reacting 2,3-dichloro-1-propene with phenol deriv. in a solvent i.e. DMF, THF, acetonitrile in the presence of base i.e. Na2CO3, NEt3, DBU at 100-200 deg. C to prep. 2- cholro-3-aryloxy-1-propene; (b) reacting with MeOH and N- bromosuccinimide to provide alpha-bromogamma-aryloxypropanone dimethyl ketal and acid-hydrolysing; (c) reacting with amidinothiourea to obfain 2-guanidino-4-aryloxymethylthiazole; and (d) reacting with beta-cyanoethylthiolate in a nonprotonic solvent i.e. DMF, DMSO at 100-110 deg. C.
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