Synthetic method of (S)-N,N-dimethyl-3-hydroxyl-3-(2-thiophen)propanamine



The invention provides a method for synthesizing (S)-N, N-dimethyl-3-hydroxyl-3-(2-thienyl) propylamine, and relates to a key intermediate of (S)-duloxetine. The method for synthesizing the (S)-N, N-dimethyl-3-hydroxyl-3-(2-thienyl) propylamine comprises the following steps: dissolving chiral diaminodiphosphine-ruthenium catalyst (III) in an organic solvent under nitrogen atmosphere; respectively adding organic hydrogen source isopropanol and an alkaliferous solution, and adding 3-dimethylamino-1-(2-thienyl)-1-acetone (II) to the mixed solvent at a temperature of between 20 and 82 DEG C so as to react to obtain the target product (S)-N, N-dimethyl-3-hydroxyl-3-(2-thienyl) propylamine (I). The method has the advantages of mild reaction condition, simple and safe operation, easy synthesis of the chiral catalyst and low cost, and the enantioselectivitiy of the product reaches 98 percent ee, and the optical purity of the product can be compared favorably to a split method. The invention provides a new effective and feasible way for industrial production of (S)-duloxetine.




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    CN-102532097-AJuly 04, 2012华东理工大学Asymmetric synthesis method of duloxetine intermediate-(S)-N, N-dimethyl-3-hydroxy-3-(2-thienyl)-1-propylamine