Acryloyl chloride → Hydrochloric Acid

Participants

Reaction Steps

To a solution of (R)-5-(4-(morpholine-4-carbonyl)phenylamino)-3-(pyrrolidin-3-ylamino)-1,2,4-triazine-6-carboxamide (83) HCl salt (60 mg, 0.13 mmol) in NMP (4 mL) was added DIEA (160 μL, 0.90 mmol) and then acryloyl chloride (25 μL, 0.30 mmol). The mixture was stirred at RT for 30 min, quenched with TFA (0.2 mL), diluted with 2 mL water, and subjected to reverse phase preparative HPLC to afford the title compound (84) as an HCl salt. MS found for C22H26N8O4 as (M+H)+ 467.1, (M−H)− 465.2. UV: λ=242 nm.

Provenance & Evidence