反应详情

A mixture of 4-(5-chloro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (100 mg), 2-fluoro-4-(methanesulfonyl)phenylboronic acid (97 mg), 2 M aqueous Na2CO3 solution (0.33 mL), methanol (0.5 mL), and 1,4-dioxane (1.5 mL) is sparged with Ar for 10 min. PdCl2 [1,1′-bis(diphenylphosphino)-ferrocene]*CH2Cl2 complex (22 mg) is added and the mixture is stirred at reflux temperature for 2 h. The mixture is diluted with water and methanol and purified by HPLC on reversed phase (methanol/water) to give the title compound. LC (method 5): tR=1.29 min; Mass spectrum (ESI+): m/z=475 [M+H]+.

1. customis sparged with Ar for 10 min
2. additionPdCl2 [1,1′-bis(diphenylphosphino)-ferrocene]*CH2Cl2 complex (22 mg) is added
3. temperatureat reflux temperature for 2 h
4. additionThe mixture is diluted with water and methanol
5. custompurified by HPLC on reversed phase (methanol/water)