An efficient one-pot conversion of Boc-protected adenines to N-6-ureas

作者：Machicao Paulo A; Peterson Matt A^*; Schols Dominique

来源：Tetrahedron Letters, 2015, 56(47): 6574-6576.

DOI：10.1016/j.tetlet.2015.10.021

• Boc-protected adenine
• N-6-Ureas
• Urea synthesis
• Purine derivatives
• Purine libraries

Treatment of Boc-protected N-9-aryladenines with 1 degrees alkylamines (1.1 equiv) and DMAP (1.1 equiv) in DMF at 80 degrees C in the presence of activated 5 angstrom 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 mu M).

• 出版日期2015-11-25
• 单位河北医科大学