Triphenylphosphine → HCID 178527243, compound

Participants

Reaction Steps

N-(1-Benzhydrylazetidin-3-yl)-N-(3,5-difluorophenyl)methylsulfonamide may be obtained by carrying out the procedure as in Example 13 (method 2) in the following manner: 0.86 g of N-(3,5-difluorophenyl)methylsulfonamide, 3.28 g of triphenylphosphine and then 2 ml of diethyl azodicarboxylate are added successively to a solution of 2 g of 1-benzhydrylazetidin-3-ol in 100 cm3 of tetrahydrofuran. An increase in the temperature, which passes from 22° C. to 29° C., as well as the formation of a precipitate immediately following the addition of the diethyl azodicarboxylate are observed. After 20 h at 22° C., the precipitate is removed by filtration and the filtrate is concentrated to dryness at 40° C. under 2.7 kPa. The residue is triturated with 5 cm3 of methanol for 20 minutes at 21° C., providing 1.07 g of N-(1-benzhydrylazetidin-3-yl)-N-(3,5-difluorophenyl)methylsulfonamide in the form of a white amorphous solid.

Provenance & Evidence