38730-39-1Relevant articles and documents
Synthesis of deuterated benzopyran derivatives as selective COX-2 inhibitors with improved pharmacokinetic properties
Zhang, Yanmei,Tortorella, Micky D.,Wang, Yican,Liu, Jianqi,Tu, Zhengchao,Liu, Xiaorong,Bai, Yang,Wen, Dingsheng,Lu, Xin,Lu, Yongzhi,Talley, John J.
, p. 1162 - 1166 (2014/12/10)
We designed a series of specifically deuterated benzopyran analogues as new COX-2 inhibitors with the aim of improving their pharmacokinetic properties. As expected, the deuterated compounds retained potency and selectivity for COX-2. The new molecules possess improved pharmacokinetic profiles in rats compared to their nondeuterated congeners. Most importantly, the new compounds showed pharmacodynamic efficacy in several murine models of inflammation and pain. The benzopyran derivatives were separated into their enantiomers, and the activity was found to reside with the S-isomers. To streamline the synthesis of the desired S-isomers, an organocatalytic asymmetric domino oxa-Michael/aldol condensation reaction was developed for their preparation.
Selective para-Bromination of Phenols via a Regenerable Polymer-bound Tetraalkylammonium Tribromide
Smith, Keith,James, D. Martin,Matthews, Ian,Bye, Martin R.
, p. 1877 - 1878 (2007/10/02)
Amberlyst-A26 resin in its tribromide form effects para-bromination of phenols with high yields and selectivity; the resin is easily recovered by filtration and can be reconverted into the tribromide form by addition of bromine.
Halogenation Using Quaternary Ammonium Polyhalides. IV. Selective Bromination of Phenols by Use of Tetraalkylammonium Tribromides
Kajigaeshi, Shoji,Kakinami, Takaaki,Okamoto, Tsuyoshi,Nakamura, Hiroko,Fujikawa, Masahiro
, p. 4187 - 4189 (2007/10/02)
Reaction of phenols with calculated amounts of benzyltrimethylammonium tribromide or tetrabutylammonium tribromide in dichloromethane-methanol for 0.5-1 h under mild conditions gave, selectively, the objective mono-, di-, or tribromophenols in good yields.
