3,5-DIARYL-4-TRIFLUOROMETHYLSULFONYL PYRAZOLE AND 1-TRIFLUOROMETHYLSULFONYL PYRAZOLO5,1-aISOQUINOLINE AND METHOD FOR PRODUCING THEM

摘要

PROBLEM TO BE SOLVED: To provide a 3,5-diaryl-4-trifluoromethylsulfonyl pyrazole and a 1-trifluoromethylsulfonyl pyrazolo[5,1-a]isoquinoline, and methods for producing them.;SOLUTION: A 3,5-diaryl-4-trifluoromethylsulfonyl pyrazole, which constitutes a group of new compounds, is successfully obtained with a high yield by using an alkynyl trifluoromethylsulfone and a hydrazonyl chloride as reactive substrates and conducting a 1,3-dipolar cycloaddition reaction in the presence of a base. Furthermore, a 1-trifluoromethylsulfonyl pyrazolo[5,1-a]isoquinoline, which constitutes a group of new compounds, is successfully synthesized with a high yield by using an alkynyl trifluoromethylsulfone and a C-N cyclic azomethineimine as reactive substrates and conducting a 1,3-dipolar cycloaddition reaction/oxidative aromatization.;COPYRIGHT: (C)2014,JPO&INPIT