Dimethylamine → HCID 59072825, compound

Participants

Reaction Steps

A mixture of 5 g of (2S)-1-(tert-butoxycarbonyl)-2,3-dihydro-1H-indole-2-carboxylic acid (commercial) and of 5.8 g of triethylamine in 100 ml of DCM is cooled in an ice bath, 8.4 g of BOP are added and the mixture is left stirring for 15 minutes. Dimethylamine gas is then added by sparging for 10 minutes and the mixture is left stirring for 3 hours at AT. The reaction mixture is concentrated under vacuum, the residue is extracted with AcOEt, the organic phase is washed with water, with a 5% Na2CO3 solution and with a 5% KHSO4 solution and dried over Na2SO4, and the solvent is evaporated under vacuum. The residue is chromatographed on silica gel, elution being carried out with a DCM/AcOEt (85/15, v/v) mixture. 4.1, g of the expected product are obtained.

Provenance & Evidence