Antibacterial compounds of formula (I) are provided, as well as stereoisomers and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
Regiocontrolled Palladium-Catalyzed Arylative Cyclizations of Alkynols
作者:Daishi Fujino、Hideki Yorimitsu、Atsuhiro Osuka
DOI:10.1021/ja5029028
日期:2014.4.30
Tuning the reactivity of arylpalladium intermediates enables control of catalyticarylative 5-exo and 6-endo cyclizations of alkynols. The two modes of cyclizations represent a rare example of controllable, regioselective difunctionalization of alkynes. The cyclizations are useful in offering a divergent synthesis of oxygen-containing heterocycles, which is of synthetic use for further derivatization
[EN] TRIAZOLYL DERIVATIVES AS SYK INHIBITORS<br/>[FR] DÉRIVÉS TRIAZOLYLE EN TANT QU'INHIBITEURS DE LA SYK
申请人:MERCK SHARP & DOHME
公开号:WO2014048065A1
公开(公告)日:2014-04-03
Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
yield. pyEDOT features an ethynyl group on its ethylenedioxy bridge, allowing further functionalization by alkyne chemistry. Its usefulness is demonstrated by a series of functionalized polythiophene derivatives that were obtained by pre- and post-electropolymerization transformations, provided by the synthetic ease of the Sonogashira coupling and click chemistry.
Studies in marine cembranolide synthesis: A synthesis of 2,3,5-trisubstituted furan intermediates for lophotoxin and pukalide
作者:Ian Paterson、Gardner Mark、Bernard J Banks
DOI:10.1016/s0040-4020(01)81102-9
日期:1989.1
Pd(0)-catalysed coupling between various furyl zinc or tin compounds and vinyl iodides is demonstrated to be a versatile method for the synthesis of 2,3-dialkyl-5-alkenylfurans like 3, as potential precursors of the ring system of lophotoxin and pukalide. A possible cyclisation substrate was successfully prepared by glycol cleavage, 21 → 24, when alcohol oxidation failed.