METHODS FOR PRODUCING VILOXAZINE SALTS AND NOVEL POLYMORPHS THEREOF

PROBLEM TO BE SOLVED: To provide methods of producing viloxazine or pharmaceutically acceptable salts thereof.SOLUTION: A method of producing viloxazine or pharmaceutically acceptable salts thereof comprises: (a) reacting 1-(2-ethoxyphenoxy)-2,3-epoxypropane with N-benzyl-aminoethanol to form a diol compound of the formula in the figure, where Et is an ethyl group and Bn is a benzyl group; (b) contacting the diol compound in a solvent system with a base and a cyclization agent to produce N-benzyl viloxazine of the formula in the figure; and (c) removing the benzyl group from the N-benzyl viloxazine.SELECTED DRAWING: Figure 4 【課題】ビロキサジン又はその薬学的に許容される塩を製造する方法の提供。【解決手段】（ａ）１−（２−エトキシフェノキシ）−２，３−エポキシプロパンとＮ−ベンジルアミノエタノールを反応させて、下記式のジオール化合物を作製し、［Ｅｔはエチル基；Ｂｎはベンジル基］、（ｂ）溶媒系において、該ジオール化合物を塩基及び環化剤と接触させて、下記式のＮ−ベンジルビロキサジンを製造し、及び（ｃ）該Ｎ−ベンジルビロキサジンからベンジル基を除去して、ビロキサジン又はその薬学的に許容される塩を製造する方法。【選択図】図４