title: Practical and cost-effective manufacturing route for the synthesis of a β-lactamase inhibitor.
abstract: 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.
authors: Process Chemistry, Merck Research Laboratories , P.O. Box 2000, Rahway, New Jersey 07065, United States.
authors: Steven P
authors: SP
authors: Miller
authors: Yong-Li
authors: YL
authors: Zhong
authors: Zhijian
authors: Z
authors: Liu
authors: Michael
authors: M
authors: Simeone
authors: Nobuyoshi
authors: N
authors: Yasuda
authors: John
authors: J
authors: Limanto
authors: Zheng
authors: Z
authors: Chen
authors: Joseph
authors: J
authors: Lynch
authors: Vincent
authors: V
authors: Capodanno
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D053961:Azabicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011083:Polycyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D053961:Azabicyclo Compounds; D004791:Enzyme Inhibitors; D011083:Polycyclic Compounds; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases; C568736:relebactam