Cesium carbonate → HCID 131723686, compound

Participants

Reaction Steps

Prepared according to the method described in Example 41b from 4-bromo-2-chloro-N-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-benzamide (0.25 g, Example 41a), 3-amino-1-pyrrolidinecarboxylic acid, 1,1-dimethylethyl ester (0.182 g, Journal of Medicinal Chemistry, 1998, 41 (22), 4273-4278), cesium carbonate (0.347 g), (R)-(+)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (0.036 g), palladium (II) acetate (0.009 g) and anhydrous toluene (3 ml). The residue was purified by HPLC eluting with a gradient of 0-5% ethanol in dichloromethane. The product was dissolved in methanol and stirred at room temperature for 3 h in the presence of 4N hydrochloric acid solution in dioxane (2 ml). The solution was concentrated under reduced pressure and triturated with diethyl ether to give the title compound as a white powder (0.057 g).

Provenance & Evidence