2,4,5-Trichloropyrimidine → HCID 86674892, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-ethynyl-piperidine-1-carboxylic acid tert-butyl ester (1.73 g), 2,4,5-trichloro-pyrimidine (0.86 mL), Pd(PPh3)2Cl2 (105 mg), and copper iodide (29 mg) in triethylamine (15 mL) under an argon atmosphere is heated in a microwave oven at 100° C. for 40 min. The solvent is evaporated in vacuo and 1 N citric acid is added. The mixture is extracted with dichloromethane and the combined extracts are washed with water, dried over MgSO4, and concentrated in vacuo. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate 85:15→80:20) to give the title compound. LC (method 7): tR=1.55 min; Mass spectrum (ESI+): m/z=356 [M+H]+.

Provenance & Evidence