Triphenylarsine → 4-Chloro-6-(1-methylpyrazol-4-yl)thieno[3,2-d]pyrimidine

Participants

Reaction Steps

A mixture of 6-bromo-4-chloro-thieno[3,2-d]pyrimidine (4.0 mmol), 1-methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (4.4 mmol), Pd2(dba)3 (0.8 mmol), Ph3As (0.8 mmol) and K2HPO4(8.0 mmol) in a DMF (40 mL) and water (10 mL) are stirred at room temperature until the reaction was complete. The reaction is partitioned between EtOAc and water, washed with brine, dried, concentrated and purified by flash column chromatography on silica gel to give 4-chloro-6-(1-methyl-1H-pyrazol-4-yl)-thieno[3,2-d]pyrimidine (compound 58.4).

Provenance & Evidence