A Convenient Way to Prepare the Key Intermediate 3-Aminomethyl-3-methyl-4-(methoxy-imino)pyrrolidine Dihydrochloride of DW286: A New Naphthyridone Antibacterial

摘要

We report herein a convenient way to prepare the key intermediate 3-aminomethy l-3-methyl-4-(methoxyimino)pyrrolidine dihydrochloride of DW286, a new fluoronaphthyridone antibacterial agent, via a 4-step sequence in an overall yield of 56 %. In this procedure, it was crucial that selective reduction of the cyano group of the cyano ketone (5) was done successfully using 5 % Pd/C as the catalytic hydrogenation.