2,4-Dichloropyrimidine → 2-Chloro-4-[(S)-3-(2-chloro-benzenesulfonyl)-pyrrolidin-1-yl]-pyrimidine

Participants

Reaction Conditions

Reaction Steps

(S)-3-(2-Chloro-benzenesulfonyl)-pyrrolidine TFA salt (250 mg) was dissolved in ACN (3.0 mL). 2,4-Dichloropyrimidine (155 mg), TEA (0.39 mL) and KF (4 mg) were added to the solution. The reaction mixture was stirred at 150° C. in the microwave oven for 2 h. The reaction mixture was evaporated to dryness and purified with preparative HPLC to yield 2-Chloro-4-[(S)-3-(2-chloro-benzenesulfonyl)-pyrrolidin-1-yl]-pyrimidine (91 mg, 36%) as a light yellow solid. MS: m/z=358.0 [M+H]+.

Provenance & Evidence