Water → 5-Chloro-thiophene-2-carboxylic acid [(S)-2-amino-3-((S)-3-methyl-morpholin-4-yl)-3-oxo-propyl]-amide

Participants

Reaction Conditions

Reaction Steps

Intermediate 2 (306 mg, 0.708 mmol) from step 1.2 was dissolved in 3 ml of DCM, cooled to 0° C. and slowly treated with 1.42 ml (1.42 mmol) of a BBr3-solution (1M in DCM). After 2 h at 0° C. 7 ml sat. aq NaHCO3-solution and 3 ml H2O were added and the reaction was stirred for 15 min at RT. The organic layer was separated and the aqueous phase extracted with DCM. The combined organic layers were washed with H2O, dried with MgSO4, filtered and evaporated to dryness. 191 mg of crude product were obtained and used without further purification in step 1.8.

Provenance & Evidence