| 摘要 |
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 (R<1> is 1-4C alkyl) and a compound of formula II [X is Cl or Br; R<2> is 1-4C alkyl; Y is CN, COR<3> (R3 is 1-4C alkyl or 6-14C aryl), or COOR<4> (R<4> is 1-4C alkyl)] are made to react in a solvent (e.g. benzene, THF etc.) or in the absence of a solvent at 50-100 deg.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 0-35 deg.C to give a compound of formula III (e.g. 1-amino-2-cyano-1,2-dimethoxycarbonylethylene). |
