Tert-butyl 3,3-difluoro-[1,3'-biazetidine]-1'-carboxylate → 3,3-Difluoro-1,3'-biazetidine

Participants

Reaction Steps

A 10 mL round-bottomed flask was charged with a solution of 3,3-difluoro-[1,3′]biazetidinyl-1′-carboxylic acid tert-butyl ester (0.15 g, 0.61 mmol) in DCM/TFA (3 mL/3 mL) The reaction mixture was stirred for 3 h at room temperature. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH and the desired product was eluted using 2 M NH3 in MeOH to give 3,3-Difluoro-[1,3′]biazetidinyl as a colourless oil (0.033 g, 37%). 1H NMR (300 MHz, CDCl3): δ 3.73-3.55 (m, 8H), 3.57-3.43 (m, 1H), 2.77 (s, 1H)

Provenance & Evidence