3,3-DIFLUOROAZETIDINE HYDROCHLORIDE synthesis

Yield:288315-03-7 80.1%

Reaction Conditions:

with hydrogen in methanol at 40; under 2585.81 Torr;

Steps:

9.2 3,3-difluoroazetidine hydrochloride
Under an argon atmosphere, Pd / C (1.0g, 33% / W) was added to the 15-2 (3.0g, 11.58mmol) in methanol (30 mL) solution, vacuum degassing, washed several times with hydrogen.The mixture under hydrogen (50 psi for) atmosphere, and stirred overnight at 40 deg.] C, TLC (petroleum ether: ethyl acetate = 10) to monitor the end of the reaction, after filtration, to the residue was added dropwise to HCl / MeOH solution, the organic layer was reduced pressure and concentrated to give a yellow solid 15-3 (1.2g, 80.1%).

References:

KBP BIOSCIENCES CO LTD;ZHANG, HUI CN103635456, 2016, B Location in patent:Paragraph 0336-0338

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