1-Propanol → HCID 9800958, compound

Participants

Reaction Steps

A stirred solution of 2-[(S)-1-phenylethylamino]-4-[5-iodobenzimidazol-1-yl]pyrimidine (EXAMPLE 271) (37 mg), 3-thiophene boronic acid (16 mg), K2CO3 (35 mg) and Pd(PPh3)4 (0.97 mg) in 1:1 n-propanol:water (4 mL) was stirred under N2 at 100° C. for 16 h. The reaction mixture was cooled and poured into 100 mL EtOAc and washed with water, then brine. The organic layer was dried over anhydrous MgSO4, filtered and concentrated under reduced pressure. The product was purified by silica gel chromatography eluting successively with 10% acetone/hexanes, 20% acetone/hexanes and 30% acetone/hexanes giving 25.3 mg of the title compound. Mass spectrum (ESI): 398.1 (M+1).

Provenance & Evidence