| 摘要 |
<p>Azidoisothiazoles (I):- (where R is halogen, SR1, SOR1 or SO2R1 and R1 is 1-12 C (iso)alkyl, benzyl or phenethyl opt. mono- or poly-substd. in nucleus by NO2 and/or halogen) have antimicrobial activity against gram + ve and -ve bacteria, and antimycotic activity and can be used as active ingredients in compsns. for treating pyrodermia, follicles, infected wounds, burns and dermatitis. They are prepared (a) by reacting: (where Y is halogen, such as Cl or Br, or a diazonium cation) with a metal azide, such as NaN3, in a polar solvent, esp. at 0-50 degrees C in water, aliphatic alcohols, DMF or DMSO, acetone, dioxan and/or TFH; or (b) by diazotising (II) where Y is hydrazino group, in acid solution.</p> |
