Tomohisa Yasuhara

An activated phosphate for an efficient amide and peptide coupling reagent

Activation of diethyl phosphate was realized by attaching trifluoromethanesulfonanilide as an efficient leaving group and the phosphate 1 proved to be a promising amide and peptide coupling reagent.

FIRST TOTAL SYNTHESIS OF CRISPINE B BY NITRO ALDOL AND THE BISCHLER-NAPIERALSKI REACTION

A pyrrolo[2,1-a]isoquinoline alkaloid, crispine B, was firstly synthesized in 55% overall yield from 3,4-dimethoxyaldehyde via five steps by employing nitro-aldol reaction and the Bischler-Napieralski reaction.

Chemoselective alkoxycarbonylation reagent having trifluoromethylsulfonyl-4-trifluoromethylanilide as a leaving group†

N-Benzyloxy- and N-tert-butoxycarbonyltrifluoromethylsulfonyl-4-trifluoromethylanilides were prepared and were found to be chemoselective and shelf-storable alkoxycarbonylation reagents.