Cesium carbonate → Trifluoroacetic acid

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-amino-6′-bromo-1-methyl-2′-phenylspiro[imidazole-4,4′-thiochroman]-5(1H)-one TFA salt (20 mg, 0.036 mmol), 3-cyanophenylboronic acid (7 mg, 0.047 mmol) and Cs2CO3 (30 mg, 0.092 mmol) in 1,4-dioxane (4 mL) and H2O (0.5 mL) charged in a 10 mL CEM microwave test tube was added PdCl2(PPh3)2 (3 mg, 0.004 mmol), then the system was degassed by sweeping N2. The tube was capped and heated to 110° C. for 10 min in a CEM microwave reactor. Solvent was removed in vacuum and the residue was purified by preparative HPLC to yield 4 isomers of the desired product as a TFA salt.

Provenance & Evidence