| 摘要 |
<p>Macrolide antibiotics of the formula: …<CHEM>… and their pharmaceutically-acceptable acid-addition salts, wherein R<1> is hydrogen or methyl; and R<2> and R<3> are each hydrogen, amino, NH-CO-R<5> or NH-SO2-R<6>; provided that one of R<2> and R<3> is always hydrogen, but R<2> and R<3> are not both hydrogen;… wherein:… (i) R<5> is selected from …<CHEM>… wherein Alk is alkyl having from 1 to 8 carbons; Ar<1> is thienyl, furyl, isoxazolyl, pyridyl, pyrazinyl or pyrimidyl; X<1> is hydrogen, fluoro, chloro, bromo, hydroxy, amino, nitro, trifluoromethyl, alkyl having 1 to 3 carbons or alkoxy having 1 to 3 carbons; X<2> is hydrogen, fluoro, chloro or bromo; n is 0 or 1; and m is 0, 1, 2 or 3; and… (ii) R<6> is selected from the group consisting of …<CHEM>… wherein Ar<2> is thienyl or furyl and X<3> is hydrogen, chloro, bromo or iodo. …<??>Also included are certain novel intermediates useful in preparing said antibiotics.</p> |
