Process Chemistry, Merck Research Laboratories , P.O. Box 2000, Rahway, New Jersey 07065, United States.
Org Lett. 2014 Jan 3;16(1):174-7. doi: 10.1021/ol4031606. Epub 2013 Dec 13.
Compound 1, a potent and irreversible inhibitor of β-lactamases, is in clinical trials with β-lactam antibiotics for the treatment of serious and antibiotic-resistant bacterial infections. A short, scalable, and cost-effective route for the production of this densely functionalized polycyclic molecule is described.
化合物 1 是一种强效且不可逆的β-内酰胺酶抑制剂,正在与β-内酰胺类抗生素联合进行临床试验,以治疗严重的和耐抗生素的细菌感染。本文描述了一种生产这种多环分子的短、可扩展且具有成本效益的路线。