Hydrochloric Acid → HCID 58504790, compound

Participants

Reaction Steps

A biphasic suspension of [(2S,5R)-4-(2-amino-6-chloro-4-pyrimidinyl)-5-methyl-2-morpholinyl]methyl phenylcarbamate (123 mg, 0.326 mmol), (4-cyano-3-fluorophenyl)boronic acid (107 mg, 0.651 mmol), PdCl2(dppf).CH2Cl2 adduct (13.3 mg, 0.016 mmol), 2N aqueous K2CO3 (0.488 mL, 0.977 mmol), and 1,4-dioxane (3 mL) was heated in a microwave reactor for 10 minutes at 140° C. The reaction was poured into 0.1 N HCl (30 mL) and CH2Cl2 (50 mL) and the aqueous was extracted with CH2Cl2 (2×50 mL). The combined organics were dried over Na2SO4, and concentrated to yield the title compound (151 mg) as a dark brown oil. LC-MS (ES) m/z=463 [M+H]+.

Provenance & Evidence