PURPOSE: To obtain the titled compound, useful as an intermediate of pharmaceuticals, agricultural chemicals, etc., without using a base, by the reaction of a cyanoformate and a halo (active methylene) compound in the presence of Zn followed by treatment with water or an acidic aqueous solution.
CONSTITUTION: A compound of formula I (R1 is 1W4C alkyl) and a compound of formula II [X is Cl or Br; R2 is 1W4C alkyl; Y is CN, COR3 (R3 is 1W4C alkyl or 6W14C aryl), or COOR4 (R4 is 1W4C alkyl)] are made to react in a solvent (e.g. benzene, THF etc.) or in the absence of a solvent at 50W100°C in the presence of Zn (preferably Zn activated with Cu). The product obtained is treated with water or an acidic aqueous solution (e.g. hydrochloric acid, sulfuric acid, etc.) at 0W35°C to give a compound of formula III (e.g. 1-amino-2-cyano-1,2-dimethoxycarbonylethylene).
KITA JIYUNICHIROU
JIBIKI HIROSHI
KAKEYA NOBORU
FUJIMURA SUSUMU
OKIMOTO KIYOMI
