Author/Authors :
Cole، نويسنده , , Andrew G. and Metzger، نويسنده , , Axel and Ahmed، نويسنده , , Gulzar and Brescia، نويسنده , , Marc-Raleigh and Chan، نويسنده , , Ray J. and Wen، نويسنده , , James and O’Brien، نويسنده , , Linda and Qin، نويسنده , , Lan-Ying and Henderson، نويسنده , , Ian، نويسنده ,
Abstract :
A general and efficient solid-phase synthesis of N-9-substituted 2,8-diaminopurines from 5-nitrouracil is described. The key synthetic transformation employs a carbodiimide-mediated cyclization of a thiourea. Thiourea formation on solid phase is performed using both thermal and microwave reaction conditions. Regiospecific solution-phase synthesis of key building blocks allows the incorporation of desired substituents at N-9 of the purine nucleus.
