Preparation of acyclo nucleoside phosphonate analogues based on cross-metathesis

作者：Kumamoto Hiroki; Topalis Dimitri; Broggi Julie; Pradere Ugo; Roy Vincent; Berteina Raboin Sabine; Nolan Steven P; Deville Bonne Dominique; Andrei Graciela; Snoeck Robert; Garin Daniel; Crance Jean Marc; Agrofoglio Luigi A^*

来源：Tetrahedron, 2008, 64(16): 3517-3526.

DOI：10.1016/j.tet.2008.01.140

In our on-going program targeting anti-pox activity, we report here the synthesis of hitherto unknown acyclic nucleoside phosphonates using olefin cross-metathesis (CM) as a key assembly step. Modification at the C-5 position of the uracil moiety was performed under optimized Pd(0)-catalyzed Stille cross-coupling conditions. None of the obtained compounds were active against poxviruses, nor do they exhibit any toxicity.

• 出版日期2008-4-14