Diisopropylethylamine → 3-(Methylcarbamoyl)isoxazol-5-ylmethyl 7-[5-(4-fluorophenyl)pyridin-2-yl]-7-azaspiro[3.5]non-2-ylcarbamate

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Reaction Steps

The process is performed according to the procedure described in Example 1, step 1.1. Starting with 1.08 g (3.47 mmol) of 7-[5-(4-fluorophenyl)pyridin-2-yl]-7-azaspiro[3.5]non-2-ylamine, described in the preceding step (step 10.5.), 1.34 g (4.16 mmol) of 3-(methylcarbamoyl)isoxazol-5-ylmethyl 4-nitrophenyl carbonate, obtained in step 4.1., 1.12 g (8.67 mmol) of N,N-diisopropylethylamine and 0.212 g (1.73 mmol) of N,N-dimethylaminopyridine, and after purification by chromatography on silica gel, eluting with a 98/2 mixture of dichloromethane and methanol, 0.847 g of pure product is thus obtained in the form of a white solid.

Provenance & Evidence