Patent ID: 6268535
Filing Date: 2001-07-31
Classification: C07B,C07C,C12C

Abstract:
A method of preparing a 3-aryl-1-indanamine represented by the following structural formula: ##STR13##and physiologically acceptable salts thereof, wherein:ring A is substituted or unsubstituted;R.sup.1 is a substituted or unsubstituted aromatic group;R.sup.2 and R.sup.3 are each, independently, hydrogen, an aliphatic group, a substituted aliphatic group, an aromatic group, a substituted aromatic group, an aralkyl group, a substituted aralkyl group, orR.sup.2 and R.sup.3, taken together with nitrogen, form a non-aromatic ring system having 1-2 heteroatoms, said method comprising the steps of:a) reacting, in the presence of a first Friedel-Crafts catalyst and a proton source, a substituted or unsubstituted benzene having at least two consecutive unsubstituted aromatic carbons, and a starting material represented by the following structural formula: ##STR14##thereby forming a 3-aryl-3-phenyl-1-propanoic acid represented by the following structural formula: ##STR15##b) contacting said 3-aryl-3-phenyl-1-propanoic acid with a second Friedel-Crafts catalyst, thereby forming a 3-arylindan-1-one represented by the following structural formula: ##STR16##c) reacting said 3-arylindan-1-one with a reducing agent, thereby forming a 3-arylindan-1-o1 represented by the following structural formula: ##STR17##d) reacting said 3-arylindan-1-o1 with an activating agent in the presence of a base, thereby forming an activated 3-arylindan-1-o1; ande) reacting said activated 3-arylindan-1-o1 with an amine compound represented by the following structural formula: ##STR18##thereby forming said 3-aryl-1-indanamine.