Water → HCID 86685973, compound

Participants

Reaction Conditions

Reaction Steps

6-Chloro-2-(5-chloromethyl-pyridin-3-yl)-3,4-dihydro-2H-isoquinolin-1-one (example 140 [A]) (75 mg, 0.25 mmol), Pd(PPh3)2Cl2 (18 mg, 0.025 mmol), Na2CO3 (80 mg, 0.75 mmol) and 3,5-dimethylisoxazole-4-boronic acid (45 mg, 0.32 mmol) were dissolved in dioxane (4.0 mL). The resulting reaction mixture was heated at 120° C. for 3 hours before it was poured into H2O (50 mL) and extracted with EtOAc (2×125 mL). The combined organic layers were washed with brine, dried over anhy. Na2SO4, filtered and concentrated in vacuo to give a crude product which was then purified by prep-HPLC to give title compound (10 mg, 10.9%) as a light yellowish solid. MS: 368.2 (M+H+).

Provenance & Evidence