METHODS OF MANUFACTURE AND PURPOSE OF THE SPHAELACTONE DERIVATIVE AND ITS COMPOSITE MEDICINES

摘要

1. The compound of formula (I): where: R is H, —C (O) R or —C (O) NRR, where R and R may be the same or different, R, R and R are hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, alkylaryl, arylalkyl, arylalkenyl, arylalkynyl and heterocycle; R = R represents a double bond, or R represents H, a R represents alkyl having from 1 to 8 carbon atoms and having a substituent, where the substituent is selected from cycloalkyl, heterocycloalkyl, aryl, , an amino acid fragment or -NRR, and pharmaceutically acceptable salts thereof, arr associated with an inorganic and / or organic acid and its quaternary ammonium salts formed with RZ; where R and R may be the same or different and are hydrogen, alkyl, cycloalkyl, alkyl substituted with hydroxyl, alkenyl, alkynyl, aryl, alkylaryl, arylalkyl, arylalkenyl , arylalkynyl, heterocycle, trifluoromethyl, perfluoroalkyl, cyano, cyanomethyl, carboxyl, carbamate, sulfonyl, sulfonamide or aryloxyalkyl; or R and R taken together with the N atom form a ring, preferably a 3-9 membered ring, where the ring may contain one or more substituents selected from hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, alkylaryl, arylalkyl, arylalkenyl, arylalkynyl or heterocycle; Z represents fluorine, chlorine, bromine, iodine, tosylate, methanesulfonate, benzenesulfonate, trifluoromethanesulfonate; R represents alkyl, cycloalkyl, alkyl substituted by hydroxyl, alkenyl, alkynyl, aryl, heterocycle, arylalkylalkyl alc Xi or aryloxyalkyl; inorganic or organic acid is hydrofluoric acid, hydrochloric