The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
四环素类抗生素在过去50年中在治疗传染病方面发挥了重要作用。然而,
四环素类抗生素在人类和兽医医学中的增加使用导致许多先前对
四环素类抗生素敏感的
生物产生了抗药性。最近通过手性烯酮中间体的模块化合成开发了
四环素类似物的有效合成方法,从而实现了以前从未制备过的新型
四环素类似物的合成。本发明提供了一种更有效的制备烯酮中间体的方法。