PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR

摘要

The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity.;;The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.

主权项

1. A process for preparing a compound of Formula (I): or a salt thereof, comprising: (a) reacting a compound of Formula (VI): or a salt thereof, with a compound of Formula (VII): or a salt thereof, to form a compound of Formula (III): or a salt thereof; (b) reacting a compound of Formula (IV): with a compound of Formula (V): or a salt thereof, to form a compound of Formula (II): or a salt thereof; and (c) reacting said compound of Formula (II) or a salt thereof, with said compound of Formula (III) or a salt thereof, to form said compound of Formula (I) or a salt thereof; wherein:
R1 is a halogenR2 is a leaving group; andR3 is a halogen; provided that R2 is a leaving group other than 3H-[1,2,3]triazolo[4,5-b]pyridin-3-yloxy.