Palladium(II)-catalyzed enantioselective C(sp3)-H activation using a chiral hydroxamic acid ligand
An enantioselective method for Pd(II)-catalyzed cross-coupling of methylene β-C(sp3)-H bonds in cyclobutanecarboxylic acid derivatives with arylboron reagents is described. High yields and enantioselectivities were achieved through the development of chiral mono-N-protected α-amino-O- methylhydroxamic acid (MPAHA) ligands, which form a chiral complex with the Pd(II) center. This reaction provides an alternative approach to the enantioselective synthesis of cyclobutanecarboxylates containing α-chiral quaternary stereocenters. This new class of chiral catalysts also show promises for enantioselective β-C(sp3)-H activation of acyclic amides.
Xiao, Kai-Jiong,Lin, David W.,Miura, Motofumi,Zhu, Ru-Yi,Gong, Wei,Wasa, Masayuki,Yu, Jin-Quan
supporting information
p. 8138 - 8142
(2014/06/23)
Compounds Which Selectively Modulate The CB2 Receptor
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally usefu
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Page/Page column 55-56
(2010/04/23)
Synthesis of (2-arylethylidene)cyclobutanes by palladium-catalyzed reactions of aryl halides with homoallyl alcohols bearing a trimethylene group at the allylic position
Treatment of aryl bromides with homoallyl alcohols bearing a trimethylene group at the allylic position in the presence of cesium carbonate under palladium catalysis affords (2-arylethylidene) cyclobutanes selectively. The selective formation of the alkylidenecyclobutane skeleton results from regiospecific retroallylation of the homoallyl alcohols, which accompanies the transposition of the double bonds. Georg Thieme Verlag Stuttgart.
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model.
Sun, Daqing,Wang, Zhulun,Cardozo, Mario,Choi, Rebekah,DeGraffenreid, Michael,Di, Yongmei,He, Xiao,Jaen, Juan C.,Labelle, Marc,Liu, Jinsong,Ma, Ji,Miao, Shichang,Sudom, Athena,Tang, Liang,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table
p. 1522 - 1527
(2009/12/07)
Spiro derivatives as lipoxygenase inhibitors
The present invention is concerned with certain novel spiro substituted heterocylic ring derivatives. These compounds may be useful in the manufacture of pharmaceutical compositions for treating disorders mediated by lipoxygenases. They may also be useful
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Page/Page column 93
(2008/06/13)
ARYL SULFONAMIDE COMPOUNDS AND USES RELATED THERETO
The present invention provides Aryl Sulfonamide Compounds having the formula: (I); and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, and other diseases and disorders.
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Page/Page column 74-75
(2010/02/12)
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