Pancratistatin prodrug

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

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546 23, C07F 9576, A61K 31675

Patent

active

055299890

ABSTRACT:
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: ##STR1##

REFERENCES:
patent: 4985436 (1991-01-01), Pettit
Medicinal Chemistry, The Role of Organic Chemistry in Drug Research, 2nd tion, 1993, Chapter 4, A. J. Collis, pp. 72-73.

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