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1st November 2012 @ 00:11
EDC Coupling of MNR51 with Dimethylamine to give MNR52-1

See - Synthesis of AEW16-1

Hazard Assessment


reaction on at 1045am 1/1/12

EDCI (0.083, 0.44 mmol) and HOBt (0.005 g, 0.04 mmol) were added to a solution of MNR51-1 (105 mg, 0.36 mmol) in DCM (5 mL) and the mixture was stirred for 20 minutes. Dimethylamine (~5.6 M in absolute ethanol, 0.097 mL, 0.54 mmol) was added and the reaction mixture stirred at room temperature.

After 5 h, TLC showed spot to spot conversion to another product. The reaction was poured into a saturated aqueous solution of sodium bicarbonate (8 mL), extracted with DCM (3 x 8 mL), washed with brine, dried (MgSO4), filtered and evaporated to give a yellow oil. Crude 1H NMR looked promising.