| 摘要 |
NEW MATERIAL:The compound of formula I (R<1> is H or alkyl; R<2> is H, halogen, CF3 or lower alkylthio; R<3> is H or lower alkyl) and its salt. EXAMPLE:4-(4-Chlorophenyl)-2-methyloxazole-5-propionic acid. USE:A remedy for diabetes. It has low toxicity and is effective to lower the blood level of mammals, improve the resistance to sugar, and improve the sensitivity to insulin. PREPARATION:The compound of formula I is prepared by (1) reacting the compound of formula II (X is halogen) with the compound of formula III, (2) halogenating the product to obtain the compound of formula IV, (3) reacting the compound with alpha-haloacetoacetic acid ester of formula V (R<4> is lower alkyl), (4) deacetylating the product to obtain the compound of formula VI (Z is halogen), and (5) dehalogenating the compound in a solvent in the presence of a reducing agent such as H2 or a combination of a metal with an acid, at 20-100 deg.C.
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