| 摘要 |
PURPOSE:To prepare the titled compound useful as an anti-inflammatory agent, etc. under mild condition, by reacting a specific phenyl-acetic acid derivative with halogenoacetaldehyde or its reactive derivative in the presence of an acid, and hydrolyzing the reaction product. CONSTITUTION:The objective compound of formula II can be prepared by (1) reacting the compound of formula I (A is O or S; R<1> and R<2> are H, lower alkyl or halogen; R<3> is H or lower alkyl; R<4> is lower alkyl; Y is H, cyano or lower alkoxycarbonyl) with a halogenoacetaldehyde or its reactive derivative in the presence of a catalytic amount of an anhydrous acid such as p-toluenesulfonic acid, etc., and (2) hydrolyzing the reaction product. The starting compound of formula I is obtained by reacting the hydroxy- or mercaptophenylacetic acid derivative of formula III with a halogenocyan, and reacting the resultant (thio) cyanato-phenylacetic acid derivative of formula IV with hydrogen sulfide in an ether solvent in the presence of a base.
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