4-(5-Chloro-2,3-dihydrofuro[2,3-c]pyridin-2-yl)piperidine-1-carboxylic acid tert-butyl ester → 4-[5-(2-Oxo-2H-pyrazin-1-yl)-2,3-dihydro-furo[2,3-c]pyridin-2-yl]-piperidine-1-carboxylic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-(5-chloro-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (60 mg), 2-hydroxypyrazine (17 mg), and copper iodide (7 mg) in 1,4-dioxan (1 mL) is sparged with argon. N,N′-Dimethylethylendiamine (8.54) and tri-potassium orthophosphate (72 mg) are added and the resulting mixture is heated in a microwave oven to 180° C. for 1 h. The reaction mixture is filtered and chromatographed on silica gel (ethyl acetate) to give the title compound. LC (method 7): tR=1.32 min; Mass spectrum (ESI+): m/z=399 [M+H]+.

Provenance & Evidence