4-Fluoro-3-nitrobenzenesulfonamide → 4-[[(3R)-1-(2,2-Difluoroethyl)-3-pyrrolidinyl]amino]-3-nitrobenzenesulfonamide

Participants

Reaction Steps

To a solution of EXAMPLE 407B (468 mg) in tetrahydrofuran (20 mL), N-ethyl-N-isopropylpropan-2-amine (2.193 mL) and N,N-dimethylformamide (2 mL) was added 4-fluoro-3-nitrobenzenesulfonamide (473 mg) and the reaction mixture was stirred 72 hours. The crude product was isolated by concentration and was purified on silica gel, and was eluted with a 0.5, 2.5, and 5% methanol in methylene chloride step gradient to obtain the title compound.

Provenance & Evidence