159305-15-4Relevant academic research and scientific papers
Br?nsted acid/rhodium(II) cooperative catalytic asymmetric three-component aldol-type reaction for the synthesis of 3-amino oxindoles
Ren, Lei,Lian, Xiao-Lei,Gong, Liu-Zhu
supporting information, p. 3315 - 3318 (2013/07/11)
Cooperation is key! Chiral Br?nsted acid/rhodium(II) cooperative catalysis enabled an enantioselective three-component aldol-type reaction of 3-diazo oxindoles and anilines with glyoxylates to give highly functionalized and structurally diverse 3-amino oxindoles in high stereoselectivity (>20:1 d.r., 99 % ee; see scheme). Copyright
Ru(ii)-catalyzed intermolecular ortho-C-H amidation of aromatic ketones with sulfonyl azides
Bhanuchandra,Ramu Yadav,Rit, Raja K.,Rao Kuram, Malleswara,Sahoo, Akhila K.
supporting information, p. 5225 - 5227 (2013/06/27)
Ru(ii)-catalyzed intermolecular ortho-C-H amidation of weakly coordinating aromatic ketones with sulfonyl azides is reported. The developed reaction protocol can be extended to various substituted aromatic ketones to afford a wide range of desired C-N bond formation products in good yields.
QUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS
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Page/Page column 44; 45, (2013/04/24)
This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pr
Highly stereoselective chemoenzymatic synthesis of the 3 h -isobenzofuran skeleton. access to enantiopure 3-methylphthalides
Mangas-Sanchez, Juan,Busto, Eduardo,Gotor-Fernandez, Vicente,Gotor, Vicente
supporting information; experimental part, p. 1444 - 1447 (2012/06/01)
A straightforward synthesis of (S)-3-methylphthalides has been developed, with the key asymmetric step being the bioreduction of 2-acetylbenzonitriles. Enzymatic processes have been found to be highly dependent on the pH value, with acidic conditions being required to avoid undesired side reactions. Baker's yeast was found to be the best biocatalyst acting in a highly stereoselective fashion. The simple treatment of the reaction crudes with aqueous HCl has provided access to enantiopure (S)-3-methylphthalides in moderate to excellent yields.
Discovery of a novel series of 4-quinolone JNK inhibitors
Gong, Leyi,Tan, Yun-Chou,Boice, Genevieve,Abbot, Sarah,McCaleb, Kristen,Iyer, Pravin,Zuo, Fengrong,Porto, Joseph Dal,Wong, Brian,Jin, Sue,Chang, Alice,Tran, Patricia,Hsieh, Gary,Niu, Linghao,Shao, Ada,Reuter, Deborah,Lukacs, Christine M.,Ursula Kammlott,Kuglstatter, Andreas,Goldstein, David
, p. 7381 - 7387 (2013/02/21)
A novel series of highly selective JNK inhibitors based on the 4-quinolone scaffold was designed and synthesized. Structure based drug design was utilized to guide the compound design as well as improvements in the physicochemical properties of the series. Compound (13c) has an IC50 of 62/170 nM for JNK1/2, excellent kinase selectivity and impressive efficacy in a rodent asthma model.
Antipsychotic indazole derivatives
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, (2008/06/13)
Disclosed is a class of 1H-indazole derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, which are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D4 receptor subtyp
Indazole derivatives
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, (2008/06/13)
A class of chemical compounds comprising a 1-H-indazole moiety and a substituted heterocyclic moiety, linked via the 3-position of the indazole moiety by a methylene group, are ligands for dopamine receptor subtypes within the body and are therefore usefu
