1005346-96-2Relevant articles and documents
Design and enantioselective synthesis of 3-(α-acrylic acid) benzoxaboroles to combat carbapenemase resistance
Chen, Fener,Chen, Xiao-Pan,Deng, Ji,Li, Gen,Li, Guo-Bo,Schofield, Christopher J.,Xiao, You-Cai,Yan, Yu-Hang,Yu, Jun-Lin,Zhu, Kai-Rong,Brem, Jürgen
, p. 7709 - 7712 (2021)
Chiral 3-substituted benzoxaboroles were designed as carbapenemase inhibitors and efficiently synthesisedviaasymmetric Morita-Baylis-Hillman reaction. Some of the benzoxaboroles were potent inhibitors of clinically relevant carbapenemases and restored the activity of meropenem in bacteria harbouring these enzymes. Crystallographic analyses validate the proposed mechanism of binding to carbapenemases,i.e.in a manner relating to their antibiotic substrates. The results illustrate how combining a structure-based design approach with asymmetric catalysis can efficiently lead to potent β-lactamase inhibitors and provide a starting point to develop drugs combatting carbapenemases.
Synthesis of naphthalene ring derivatives and Benzoheterocycles the method of the compound
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Paragraph 0048; 0049, (2016/10/10)
The invention discloses a method for synthesizing naphthalene derivative and benzo-heterocycle compounds. The method is realized by promoting a reaction similar to Mortia-Baylis-Hillman between aryl aldehyde having alpha, beta-unsaturated ester on ortho-position and ketone compounds under the catalysis action of tertiary amine and tertiary phosphine organic small molecular catalysts, so as to remove a molecule of H2O, so that the naphthalene derivative or benzo-heterocycle compounds are generated. The method disclosed by the invention is simple in operation step, cheap and easily available in adopted catalysts and harmless to environment, and a series of naphthalene derivative and benzo-heterocycle compounds are synthesized with relatively high yield.