|Title:|| Method of preparing 9-amino-1,2,3,4,-tetrahydroacridin-1-ones and related compounds|
|Abstract:||There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.CH where CR.sub.5 and CH correspond to Y and Z respectively; an optical antipode thereof, or a pharmaceutically acceptable acid addition salt thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.|
|Inventor(s):|| Shutske; Gregory M. (Somerset, NJ), Pierrat; Frank A. (Coventry, RI) |
|Assignee:|| Hoechst-Roussel Pharmaceuticals, Inc. (Somerville, NJ) |
|Filing Date:||Nov 25, 1987|
|Claims:||1. A method of preparing a compound of the formula ##STR20## where n is 1,2,3, and X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, which comprises cyclizing a compound of the formula ##STR21## in the presence of a metallic halide and a basic inorganic salt to obtain said compound. |
2. The method as defined in claim 1 wherein said cyclization is conducted in the presence of CuCl, CuBr or CuI used as a catlayst.