Methods for preparing naphthyridines

摘要

The present invention provides methods of synthesizing compounds of formula (1) and intermediates thereto. The present invention also provides intermediates useful in the synthesis of compounds of formula (1).;

主权项

1. A method of preparing a compound of formula (1)wherein Q is an optionally substituted N-containing heterocyclyl or optionally substituted N-containing heteroaryl, and Y is a lower alkyl group;
said method comprising:
a) treating a compound of formula (2) with an acid activating agent, a non-nucleophilic base, lower alkyl N,N-lower dialkyl aminoacrylate and lower alkylamine, under conditions sufficient to obtain a compound of formula (3)  wherein R is lower alkyl,b) reducing the nitro group of the compound of formula (3) from step (a) to obtain a compound of formula (4) c) treating the compound of formula (4) from step (b) with 2-indanone and a suitable reducing agent under conditions sufficient to obtain a compound of formula (5) d) hydrolysing the compound of formula (5) from step (c) to obtain a compound of formula (6); and e) reacting (6) with an acid activating agent and QH, under conditions sufficient to obtain a compound of formula (1).