PRODUCTION OF ALPHA-ARYLCARBONYL DERIVATIVE
摘要:
PURPOSE:To obtain the titled compound useful as an intermediate for pharmaceuticals, etc., economically, by condensing an aryl halide with an imine compound in the presence of a palladium compound, a tert-phosphine and a base and hydrolyzing the condensation product. CONSTITUTION:The objective compound of formula I useful also as an intermediate for food additives and perfumes is produced from an inexpensive raw material with simple procedure in high yield, by condensing (A) a compound of formula II (R1 and R2 are H, lower alkyl or lower alkoxy or R1 and R2 together form methylenedioxy; X is halogen) with (B) a compound of formula III (R3 and R4 are H or lower alkyl or together form a 5-7-membered cycloalkyl; R5 is lower alkyl or cyclohexyl) in the presence of a palladium compound of formula Pd(acac)2 (acac is acetylacetonate), etc., a tert-phosphine of formula V, etc., and a base such as sodium t-butyrate and hydrolyzing the condensation product.
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