New method for synthesizing an intermediate of Rivaroxaban, 4- {4 - (5S) -5- (aminomethyl) -2-oxo-1,3-oxazolidin-3-yl phenyl} morpholin-3-one

摘要

A method for synthesizing the Rivaroxaban intermediate, 4- {4 - [(5S) -5- (aminomethyl) -2-oxo-1,3-oxazolidin-3- yl] phenyl]} morpholin-3-one, selected from the following two methods: method I, comprising: step (1): the condensation of compound 1 with compound 2 to form compound 3; and step (2): deprotecting compound 3 to provide compound 4, ie 4- {4 - [(5S) -5- (aminomethyl) -2-oxo-1,3-oxazolidin-3-yl] phenyl ]} morpholin-3-one, wherein the reaction scheme is described as follows: ** Formula ** and method II, comprising: step (1): the condensation of compound 1 with compound 5 to form compound 3 ; step (2): deprotect compound 3 to provide compound 4, ie 4- {4 - [(5S) -5- (aminomethyl) -2-oxo-1,3-oxazolidin-3-yl] phenyl] } morpholin-3-one, wherein the reaction scheme is described as follows: ** Formula **