Tris(hydroxymethyl)aminomethane → HCID 59525958, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of PS-CDI (152 mg, 0.19 mmol), HOBt (14 mg, 0.091 mmol), {{[6-({3-(Aminocarbonyl)-5-[2-fluoro-4-(1-hydroxy-1-methylethyl)phenyl]-2-thienyl}amino)pyridin-2-yl]methyl}[(benzyloxy)carbonyl]amino}acetic acid (45 mg, 0.076 mmol) and 2-(methylamino)ethanol (7.0 mg, 0.091 mmol) in 2:1 mixture of DCM (1.6 mL) and DMF (0.8 mL) was heated to 100° C. under the microwave irradiation for 5 min. Upon cooling, MP-isocyanate (241 mg, 0.30 mmol), PS-trisamine (89 mg, 0.30 mmol) and 1 mL DCM were added to a reaction mixture and heated to 100° C. under the microwave irradiation for 10 min. The reaction mixture was filtered, washed with DCM, and concentrated in vacuo to afford the title compound.

Provenance & Evidence