Patent ID: 6071930
Filing Date: 2000-06-06
Classification: A61P,C07D

Abstract:
A process for making compounds of Formula I: ##STR39## wherein A is an aromatic moeity selected from the group consisting of: ##STR40## wherein: X.sub.1, X.sub.2, and X.sub.3 are each individually selected from the group consisting of C, or N;X.sub.4 and X.sub.5 are each individually selected from the group consisting of C, N, O, and S wherein at least one of X.sub.4 and X.sub.5 is N, O, or S;R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 are each independently selected from the group consisting of H, alkyl, hydroxyl, alkoxyl, aryloxyl, halo, amino, alkylamino, dialkylamino, or nitro, or alternatively, two adjacent R groups together may form a briding group selected from the group consisting of alkydienyl, alkyleneoxy, alkylenedioxy, alkyleneimine, and alkylenediimine; andthe dashed line indicates that the bond may be a double bond or a single bond,with the provisos that:when any of X.sub.1, X.sub.2, X.sub.3, X.sub.4 or X.sub.5 is C, the dashed lines connected thereto are double bonds;when any of X.sub.1, X.sub.2, or X.sub.3 is N, the dashed lines connected thereto are double bonds and the R group attached at that position is absent;when either X.sub.4 or X.sub.5 is N, the dashed lines connected thereto may be single bonds or double bonds, and when the dashed line is a double bond, the R group attached at that position is absent; andwhen either X.sub.4 or X.sub.5 is O or S, the dashed lines connected thereto are single bonds and the R group attached at that position is absent;said process comprising:(a) reacting a compound of Formula II: ##STR41## with a compound of Formula IV:A--CHO IVto produce a Schiff base intermediate of Formula VI: ##STR42## (b) cyclizing the Schiff base intermediate to give a pyridopyrimidinone intermediate of Formula V: ##STR43## and (c) thermally converting said pyridopyrimidinone intermediate to a compound of Formula I.