Andrew G. Myers,David A. Kummer,Derun Li,Evan Hecker,Amelie Dion,Peter M. Wright
申请号:
US14792493
公开号:
US09688644B2
申请日:
2015.07.06
申请国别(地区):
US
年份:
2017
代理人:
摘要:
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 more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.