| 主权项 |
1. A process for the synthesis of a compound of formula (I):wherein a compound of formula (II):is reacted with ammonia at a temperature greater than 100° C. to form a compound of formula (III):which is reduced to yield a bicyclic amine of formula (IV):which latter compound is subsequently subjected:
either to a coupling reaction, under basic conditions in a polar medium, with a compound of formula (V):wherein Y represents —CH2-Hal wherein Hal is a halogen, or a —CH2—OSO2—R group wherein R is an (C1-C6)alkyl group or a —C6H4—CH3 group,
or to reductive amination, in an acid medium, with a compound of formula (V′):wherein R′ and R″ represent, each independently of the other, a (C1-C6)alkyl group, or R′ and R″ together form a group —(CH2)n— wherein n=2-3, or one of the groups R′ and R″ represents a hydrogen atom and the other represents a (C1-C6)alkyl group,
or to reductive amination with a compound of formula (V″):to yield the free base of the compound of formula (I), which is placed in the presence of HCl to form the compound of formula (I), which is isolated in the form of a solid. |
