The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a β-, γ- or δ-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.
The present invention relates to novel amidoxime and amidine oxazolidinones of formula I , wherein R2, Y1, Y 2, Y3, X, W, G and U are as defined herein in the specification. The compounds of the present invention have potent activities against gram-positive bacteria.
Economical, Green, and Safe Route Towards Substituted Lactones by Anodic Generation of Oxycarbonyl Radicals
作者:Alessia Petti、Matthew C. Leech、Anthony D. Garcia、Iain C. A. Goodall、Adrian P. Dobbs、Kevin Lam
DOI:10.1002/anie.201909922
日期:2019.11.4
A new electrochemical methodology has been developed for the generation of oxycarbonyl radicals under mild and green conditions from readily available hemioxalate salts. Mono- and multi-functionalised γ-butyrolactones were synthesised through exo-cyclisation of these oxycarbonyl radicals with an alkene, followed by the sp3 -sp3 capture of the newly formed carbon-centred radical. The synthesis of functionalised
The present invention relates to an evaporation apparatus capable of supplying active ingredients sufficiently and stably. One embodiment of the invention comprises a retention vessel keeping a liquid formulation which contains active ingredients, a liquid absorbing mechanism which absorbs the liquid formulation from said retention vessel, an evaporation mechanism which evaporates active ingredients of said liquid formulation absorbed into said liquid absorbing mechanism and adjusting means which adjusts the evaporation of active ingredients.
The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation.