METHOD FOR PRODUCING 4, 4-DIFLUORO-3,4-DIHYDROISOQUINOLINE DERIVATIVES

摘要

Provided is a simple and efficient method for the large-scale production of a 4,4-difluoro-3,4-dihydroisoquinoline derivative. In the method for producing a 4,4-difluoro-3,4-dihydroisoquinoline derivative represented by general formula (1):;;a compound represented by general formula (2):;;is reacted with hydrogen fluoride.

主权项

1. A method for producing a compound represented by general formula (1):wherein R1 and R2 independently represent an optionally substituted alkyl group having 1 to 6 carbon atoms or R1 and R2 together with the carbon atom to which they are bound form an optionally substituted cycloalkyl group having 3 to 10 carbon atoms, X represents a halogen atom, optionally substituted alkyl group having 1 to 6 carbon atoms or optionally substituted alkoxy group having 1 to 6 carbon atoms, n represents an integer of 0 to 4, Y represents a halogen atom, optionally substituted alkyl group having 1 to 6 carbon atoms or optionally substituted alkoxy group having 1 to 6 carbon atoms, and m represents an integer of 0 to 6, comprising reacting a compound represented by general formula (2):wherein R1, R2, X, Y, n and m are the same as previously defined, with hydrogen fluoride.