Cyclopropylamine → N2-Cyclopropylpyrazine-2,3-diamine

Participants

Reaction Conditions

Reaction Steps

A glass microwave reaction vessel (20 mL) was charged with 3-chloropyrazin-2-amine (0.500 g, 3.86 mmol, FSSI), tris(dibenzylideneacetone)dipalladium(o) (0.070 g, 0.076 mmol, Strem Chemicals, Inc.) and BrettPhos (0.100 g, 0.186 mmol, Strem Chemicals, Inc.). The vessel was transferred to the glove-box where sodium tert-butoxide (0.700 g, 7.28 mmol, Sigma-Aldrich Chemical Company) was added. The vessel was capped and placed under an atmosphere of argon using 3 evacuation/backfill cycles. Dioxane (5 mL) and cyclopropylamine (0.410 mL, 5.85 mmol, Alfa Aesar) were added and the reaction mixture was heated at 45° C. for 1 h. The reaction was poured into water (100 mL, 0° C.) and the extracted with DCM (4×).

Provenance & Evidence