| 摘要 |
<p>(A) 4-Hydroxyerythromycin A derivs.: (I) E = erythronolide and cladinoside moiety R1 = Me2N, NH2 or N3 R2 = OH or R1 + R2= -O- (B) Acid-addition salts of (I) Antibiotics, esp. effective on intramuscular admin. against bacteria (I) oxidised with a peroxide and N-oxide htd. at 150-170 deg. for best yields. Product epoxidised esp. with m-chloroperbenzoic acid and opt. reacted with NaN3, producted reduced and reacted with CH2O under reducing conditions. 14 g. (IV) in CHCl2 treated during 30 mins. with 20 g. m-chloroperbenzoic acid then kept at 0 deg. for 24 hrs. Soln. washed, evapd. under red. press. and residue in 25 ml. warm acetone cooled to give 10.5 g. (74%) (I; R1+R2=0), m 221-3 deg.</p> |
