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

(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.

1. customwere provided in a glass autoclave
2. filtrationUpon completion of hydrogenation, the reaction mixture was filtered
3. customthe solvent was removed under reduced pressure

ORD record

ord-341692a30d424d8d8007e88f398ace9c

Source dataset

uspto-grants-2012_05

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US08168805B2