Process for preparing (S) - (+) - N-methyl-3- (1-naphthyloxy) -3- (2-thienyl) propylamine by using a compound of metilhidroxilaminopropanol Optically active as an intermediate

摘要

A process for preparing (S) - (+) - N-methyl-3- (1-naphthyloxy) -3- (2-thienyl) propylamine, comprising the steps of: carrying out a cleavage reaction in N, O a compound represented by formula (II), ** ** formula to form (S) - (-) - 3-methylamino-1- (2-thienyl) propan-1-ol as shown in formula ( III) ** ** Formula; and reacting the (S) - (-) - 3-methylamino-1- (2-thienyl) propan-1-ol with 1-halonaftaleno excess to form (S) - (+) - Nmetil- 3- (1 -naftiloxi) -3- (2-thienyl) propylamine represented by the following formula, formula ** ** wherein R is a hydrogen atom, C1-8 alkyl or C6-10 aryl; and halo is F, Cl, Br or I, wherein KOR1 and DMSO used in the reaction step (S) - (-) - 3-methylamino-1- (2-thienyl) propan-1-ol with 1-halonaftaleno, and R1 is C1- 6 alkyl, and wherein DMSO is used in amounts ranging from one to five times the amount of (S) - (-) - 3-methylamino-1- (2-thienyl) propan-1-ol.