NOVEL PROCEDURE FOR THE COUPLING OF STERICALLY HINDERED ELECTRON-DEFICIENT ANILINES TO THE 6-POSITION OF THE PURINE CORE

作者：Leenders Ruben^*; Heeres Jan; Vandenput Dirk; Guillemont Jerome; Lewi Paul

来源：Synthetic Communications, 2011, 41(21): 3246-3250.

DOI：10.1080/00397911.2010.517615

• Heterocycles
• HIV
• medicinal chemistry

Sterically hindered electron-deficient anilines are coupled to the 6-position of the purine core only when activated as their corresponding TFA-amide. The free anilines did not react under all conditions tested. After aqueous work-up, the TFA-group is lost.
This procedure provides a new tool in the construction of purines functionalized with a sterically hindered electron-deficient aniline in the 6-position.

• 出版日期2011