(1R,2R)-2-(2,6-二氟苯基)环丙-1-胺

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,6-Difluorobenzaldehyde (Aldrich) was converted to cis-2-(2,6-difluorophenyl)cyclopropylamine according to Example 375 (patent application WO 93/03022) and then converted to an isothiocyanate according to Example 374 (patent application WO 93/03022). This isothiocyanate was reacted with the anion of 2-amino-5-cyanopyridine to give (+,-)-N-(cis-2-(2,6-Difluorophenyl) cyclopropyl)-N'-(5-cyanopyrid-2-yl)-thiourea. 6 mg of this compound was reacted with NBS as described in Example 4 and a final purification on alumina, resulted in 0.7 mg of the title product. Rf:0.30 Silica gel eluent:diethyl ether.