PHOSPHITE-BORANE COMPOUNDS, AND METHOD OF MAKING AND USING THE SAME

摘要

Phosphite-borane compounds of the formula wherein: each R1 is independently selected from: H; C1-C10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R4)4N+, in which the substituents R4 of the ammonium nitrogen atom are H or C1-C10 alkyl; R2 is H or C1-C10 alkyl; and R3 is CNCH2CH3+BF4-, COOH, carboxyl salts, COOR5, or CONHR5, wherein R5 is C1-C10 alkyl, alkylaryl, aralkyl, or aryl; with the proviso that if at least one of the R1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R3 may also be CN. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity. Also disclosed are various synthetic methods for making such phosphorous-boron compounds, and for formulating same in unit dosage forms as well as other pharmaceutically and pharmacologically acceptable formulations.