PROCESS FOR THE PREPARATION OF 2-(1-AZABICYCLO(2.2.2)OCT-3-YL) -2,4,5,6-TETRAHYDRO-1H-BENZ(DE)ISOQUINOLIN-1-ONE AND INTERMEDIATE PRODUCT

摘要

The invention relates to novel processes for preparing compounds of formula (2) which process comprises (A) dehydrating the compounds of formula (3), or (B) separating the compound of formula (2) into individual stereoisomers, or (C) converting the compound of formula (2) to a pharmaceutically acceptable acid addition salt, or (D) converting an acid addition salt of the compound of formula (2) into non-salt form, and of compounds of formula (1) which process comprises (A) and (B) dehydrating the compound of formula (3) and hydrogenating this compound to give a diastereomeric mixture of 1, or (C) separating the diastereomeric mixture into individual stereoisomers or mixtures of them, or (D) converting the compound of formula (1) to a pharmaceutically acceptable acid addition salt, or (E) converting an acid addition salt of the compound of formula (1) to non-salt form. The invention relates also to the novel compound of formula (3) and to a process for preparing it. The compounds of formulae (2 and 1) are potent 5-HT3 receptor antagonists and are useful for treating a condition chosen from emesis, a gastrointestinal disorder, anxiety/depressive state, and pain.