Yield:-

Reaction Conditions:

with potassium carbonate;tetrakis(triphenylphosphine) palladium⁽⁰⁾ in 1,2-dimethoxyethane;water at 120; for 0.0666667 h;Microwave irradiation;Suzuki Coupling;

Steps:

64

Then a mixture of 6-chloro-4-(2-propoxy-pyrido[3,2-c/]pyrirnidin-2-ylamine (21.2 mg), potassium carbonate (0.17 mmol), tetrakis(triphenylphosphine) palladium (10 mg) and the corresponding boronic acid or pinacol ester (0.1 mmol) in DME (1 mL) and water (0.5 mL) was heated at 12O⁰C for 4 minutes by microwave. Solvents were concentrated in vacuo and the residue was purified by RP HPLC using a C18 column with a gradient of H₂O, 0.1% TFA-acetonitrile, to provide the desired product. This procedure provided, with yields ranging from 30% to 70% depending upon the aryl group introduced at the 6- position of the pyrido[3,2-c/]pyrimidine ring, the following pure compounds which were characterized by their mass spectrum MS as indicated in table 9.

References:

WO2008/77649,2008,A1 Location in patent:Page/Page column 57-58