Methylamine → N-methyl-(3S)-3-hydroxy-3-(2-thienyl)propanamide

Participants

Reaction Conditions

Reaction Steps

23 g of methyl (3S)-3-hydroxy-3-(2-thienyl)propanoate from experiments described in the Examples 1 and [lacuna] were initially introduced, and 130 ml of a 2-molar methanolic solution of methylamine were added. This mixture is stirred at 60° C. for 4 h, cooled and then concentrated in vacuo. 24 g (purity 87%; 90% of theory) are obtained in this way. The crude product can be used as such for the next step or else recrystallized from methylene chloride and hexane. This yielded 18 g of N-methyl-(3S)-3-hydroxy-3-(2-thienyl)propanamide (75% of theory) in the form of white crystals.

Provenance & Evidence