Pancratistatin prodrug

摘要

Pancratistatin has been selected for pre-clinical development but is sparingly soluble in water. A disodium phosphate derivative has been synthesized which is water soluble and is bioequivalent thereof. The critical step in the synthesis of the phenolic phosphate was phosphorylation of 1,2,3,4-tetraacetoxy-pancratistatin with dibenzyloxy(N,N-diisopropylamido)phosphine. This pancratistatin prodrug has the structure set forth below: <IMAGE>