Author/Authors :
Guo، نويسنده , , Chuangxing and Reich، نويسنده , , Siegfried and Showalter، نويسنده , , Rich and Villafranca، نويسنده , , Ernie and Dong، نويسنده , , Liming، نويسنده ,
Abstract :
FKBP-12 inhibitors AG5473 and AG5507 were resynthesized through a more efficient 11-step sequence. The key steps involved propargyl trimethylsilane addition to an N-acyliminium ion, ozonolysis of the allene and acid-catalyzed cyclization. A mild protocol for introducing a formaldehyde moiety to an anomeric center was established. The synthetic materials were evaluated in the FKBP rotamase assay.
