Diisopropylethylamine → 3-Methylcarbamoylisoxazol-5-ylmethyl 2-[5'-(4-fluorophenyl)-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-yl]ethylcarbamate

Participants

Reaction Steps

The process is performed according to the procedure described in Example 1 (step 1.6.). Starting with 0.20 g (0.43 mmol) of 4-nitrophenyl 2-[5′-(4-fluorophenyl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-yl]ethylcarbamate, described in Example 1 (step 1.5.), 0.122 g (0.95 mmol) of N,N-diisopropylethylamine, 0.026 g (0.22 mmol) of N,N-dimethylaminopyridine and 0.074 g (0.47 mmol) of 3-methylcarbamoylisoxazol-5-ylmethanol, and after chromatography on silica gel, eluting with a 98/2/0.2 mixture of dichloromethane, methanol and 28% aqueous ammonia, 0.170 g of pure product is obtained in the form of a white powder.

Provenance & Evidence