(S)-3-methoxymethylamino-1-(2-thienyl)propan-1-ol → 3-(N-Methylamino)-1-(2-thienyl)-1-propanol, (-)-

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Reaction Steps

(S)-3-methoxymethylamino-1-(2-thienyl)propan-1-ol obtained in example 2 dissolved in 10 mL of methanol with 8 mg of Raney-nickel were provided in a glass autoclave. The resulting solution was hydrogenated at 50□ for 12 hours. Upon completion of hydrogenation, the reaction mixture was filtered and the solvent was removed under reduced pressure to obtain objective compound as a crystal compound (122 mg, 90.8% by HPLC assay, 95% ee). The crude product was further purified by re-crystallization in toluene with optical purity as high as 100% ee.

Provenance & Evidence