An efficient method for the protection of aromatic amines with benzostabase and its utility in anionic aromatic transformations
Herein we describe an efficient and generally applicable method of protecting a diverse series of aromatic amines with the 'benzostabase' group. We also demonstrate its efficient use in aromatic anionic chemistry including its utility in the anionic ortho
Lu, Erhu,Yadav, Arun,Weaver, Donald F.,Reed, Mark A.
supporting information
p. 2259 - 2262
(2013/11/06)
Pd(II)-catalyzed C-H activation/aryl-aryl coupling of phenol esters
(Chemical Equation Presented) Although nitrogen-containing group-directed cyclopalladation reactions have been well-known, Pd(II) insertion into C-H bonds promoted by coordination of an oxygen-only group to the palladium remains rather rare. In the present study, the first cyclopalladation complex formed from a simple phenol ester was characterized by X-ray crystallography. A promising protocol for the ortho C-H activation/aryl-aryl coupling of phenol esters that was not sensitive to moisture or air was then established. The utility of the reaction was demonstrated for the synthesis of useful phenol derivatives. Copyright
Xiao, Bin,Fu, Yao,Xu, Jun,Gong, Tian-Jun,Dai, Jian-Jun,Yi, Jun,Liu, Lei
supporting information; experimental part
p. 468 - 469
(2010/03/25)
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma
The discovery of a pyrrolopyrimidine class of LIM-kinase 2 (LIMK2) inhibitors is reported. These LIMK2 inhibitors show good potency in enzymatic and cellular assays and good selectivity against ROCK. After topical dosing to the eye in a steroid induced mouse model of ocular hypertension, the compounds reduce intraocular pressure to baseline levels. The compounds also increase outflow facility in a pig eye perfusion assay. These results suggest LIMK2 may be an effective target for treating ocular hypertension and associated glaucoma.
Harrison, Bryce A.,Whitlock, N. Andrew,Voronkov, Michael V.,Almstead, Zheng Y.,Gu, Kun-Jian,Mabon, Ross,Gardyan, Michael,Hamman, Brian D.,Allen, Jason,Gopinathan, Suma,McKnight, Beth,Crist, Mike,Zhang, Yulian,Liu, Ying,Courtney, Lawrence F.,Key, Billie,Zhou, Julia,Patel, Nita,Yates, Phil W.,Liu, Qingyun,Wilson, Alan G. E.,Kimball, S. David,Crosson, Craig E.,Rice, Dennis S.,Rawlins, David B.
supporting information; experimental part
p. 6515 - 6518
(2010/03/31)
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