为了合成具有抗菌活性的红霉素衍生物,本文以红霉素A为原料,合成了6-位烯丙基取代中间体12,21-双键-2’-O,4"-O-二苯甲酰基-(9S)-9-O,11—O-异丙基-6—O-烯丙基红霉素A12,得到(9S)-9-羟基-12-亚甲基衍生物6和6,7-去氢-(9S)-9-羟基-12-亚甲基衍生物11。经^13C NMR,FAB—MS确证产物结构。所得化合物进行了体外抗菌活性测定。6和11均显示出较弱的抑菌活性。
The derivatives of (9S)-9-hydroxyl-12-methylene erythromycin A were synthesized by using erythromycin A as a starting material. An intermediate (9S) -9,11-O-isopropylidene-6-O-allyl-2',4"- O-bis(benzoyl)-12,21-anhydro erythromycin A 12 was obtained. The antibacterial activity in vitro of two compounds, 6 and 11, was tested. The preliminary biological test showed that two compounds exhibited less potent antibacterial activity in vitro.