Potassium Phosphate, Tribasic → HCID 66780017, compound

Participants

Reaction Steps

A mixture of 4-[(2-bromophenyl)methyl]-2-(4-morpholinyl)[1,3]thiazolo[4,5-d]pyrimidin-7(4H)-one (120 mg, 0.295 mmol), ethylboronic acid (32.7 mg, 0.442 mmol) and potassium phosphate (125 mg, 0.589 mmol) in Toluene (2 mL) was charged into a microwave tube under N2, followed by the addition of S-Phos (12.10 mg, 0.029 mmol), and Pd(OAc)2 (3.31 mg, 0.015 mmol). The mixture was irradiated with microwave at 150° C. for 15 min. The solvent was removed and the residue was partitioned between DCM and brine. The organic layer was concentrated and the residue was purified by reverse phase HPLC (5% org˜50% org) to give the product (60 mg, 58%). LCMS (ES) m/z 357.1 (M+H)+, 1H NMR (400 MHz, CDCl3-d1)) δppm 8.50 (br, s, 1H), 7.38 (m, 1H), 7.33 (m, 1H), 7.25 (m, 1H), 7.09 (m, 1H), 5.48 (s, 2H), 3.86 (m, 4H), 3.69 (m, 4H), 2.71 (q, 2H), 1.25 (t, 3H).

Provenance & Evidence