Diisopropylethylamine → tert-Butyl 2-[(3-(methylcarbamoyl)isoxazol-5-ylmethoxycarbonylamino)methyl]-6-azaspiro[3.4]octane-6-carboxylate

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Reaction Steps

The process is performed according to the procedure described in Example 1, step 1.1. Starting with 0.24 g (1.00 mmol) of tert-butyl 2-aminomethyl-6-azaspiro[3.4]octane-6-carboxylate (isomer 2b), described in Example 9 (step 9.1.), 0.321 g (1.00 mmol) of 3-(methylcarbamoyl)isoxazol-5-ylmethyl 4-nitrophenyl carbonate, obtained in step 4.1., 0.258 g (2.00 mmol) of N,N-diisopropylethylamine and 0.012 g (0.10 mmol) of N,N-dimethylaminopyridine, and after purification by chromatography on silica gel, eluting with a 98/2 mixture of dichloromethane and methanol, 0.320 g of pure product is thus obtained in the form of an amorphous solid.

Provenance & Evidence