2-Morpholinoethylamine → (2s,3s,4r,5r)-2-(3-Ethyl-[1,2,4]oxadiazol-5-yl)-5-[6-(1-ethyl-propylamino)-2-(2-morpholin-4-yl-ethylamino)-purin-9-yl]-tetrahydro-furan-3,4-diol formate

Participants

Reaction Conditions

Reaction Steps

Intermediate 9 (0.070 g, 0.161 mmol) and 4-(2-aminoethyl)morpholine (0.106 ml, 0.807 mmol) were dissolved in DMSO (0.03 ml) and heated at 80° C. in a sealed vial (eg Reacti vial™), for 26 h, a further portion of 4-(2-aminoethyl)morpholine (0.053 ml, 0.403 mmol) was added after the first 6 h. The product was purified by Autoprep. HPLC to give the title compound after freeze drying as a beige solid (0.049 g). LC/MS system B Rt=2.27 min, m/z=532 MH+.

Provenance & Evidence