An efficient one-pot conversion of Boc-protected adenines to N6-ureas. Issue 47 (25th November 2015) - Machicao, Paulo A.
Graphical abstract: Abstract: Treatment of Boc-protected N 9 -aryladenines with 1° alkylamines (1.1 equiv) and DMAP (1.1 equiv) in DMF at 80 °C in the presence of activated 5 Å molecular sieves gave the corresponding N 6 -urea derivatives in excellent yields (66–96%). Select derivatives were screened for antiproliferative activity against a panel consisting of L1210, CEM, and HeLa cells. The most potent analogue exhibited selective activity against HeLa cells (IC50 = 11 ± 1 μM).