SIASTATIN B DERIVATIVE AS NOVEL ANTIVIRAL SUBSTANCE AND ITS PRODUCTION

摘要

NEW MATERIAL:A compound of formula I [ R is OH, alkyloxy, aralkyloxy or (substituted) amino]. EXAMPLE:4-Deoxy-4-ene siastatin B. USE:An antiviral agent. Low toxic and highly soluble to water. PREPARATION:Siastatin B of formula II is chemically transformed. For example, a compound of the formula II is dissolved in an organic solvent such as DMF, and e.g. di-tert. butyl dicarbonate, a Boc-modifying reagent, as an acylating agent, is added to the resulting solution in the presence of e.g. triethylamine followed by heating to 50-100 deg.C to form an enol compound, a novel intermediate of formula III. This compound is then dissolved in e.g. 1-4N hydrochloric acid-dioxane, and the resultant solution is left to stand at room temperature for 1-4hr to effect elimination of the amino-protective group Boc, thus obtaining the compound given in EXAMPLE.