1,3-Propanediamine → 3-(3-Amino-propylcarbamoyl)-pyrazine-2-carboxylic acid

Participants

Reaction Steps

To a solution of 2,3-pyrazinedicarboxylic anhydride (6.50 g, 43.3 mmol) in ethanol (25 mL) was added 1,3-propanediamine (3.42 g, 46.0 mmol) dropwise over 5 min. The reaction was stirred over night at RT and the precipitated product was collected by filtration to yield 9.15 g of 3-(3-Amino-propylcarbamoyl)-pyrazine-2-carboxylic acid as a white solid (94%). This intermediate (200 mg) was dissolved in DMF (3 mL) and heated in a microwave reactor for 3 min at 175° C. to produce 7,8-Dihydro-6H-1,4,5,8a-tetraaza-fluoren-9-one, which was used without further purification.

Provenance & Evidence