866029-28-9Relevant academic research and scientific papers
Enantioselective Construction of Spiro Quaternary Carbon Stereocenters via Pd-Catalyzed Intramolecular α-Arylation
Wu, Ting,Kang, Xuehua,Bai, Heng,Xiong, Wenrui,Xu, Guangqing,Tang, Wenjun,Tang, Wenjun
, p. 4602 - 4607 (2020/06/29)
We herein report the development of a sterically hindered and electron-rich P-chiral monophosphorus biaryl ligand that has enabled a general and efficient enantioselective intramolecular α-arylation, providing access to a wide series of [4.4], [4.5], and [4.6]-spirocycles with chiral benzylic quaternary carbons in high yields with good to excellent enantioselectivities. A pronounced water effect on enantioselectivity is observed.
Synthesis and inhibitory studies of phosphonic acid analogues of homophenylalanine and phenylalanine towards alanyl aminopeptidases
Wanat, Weronika,Talma, Micha?,Dziuk, B?a?ej,Kafarski, Pawe?
, p. 1 - 22 (2020/09/18)
A library of novel phosphonic acid analogues of homophenylalanine and phenylalanine, containing fluorine and bromine atoms in the phenyl ring, have been synthesized. Their inhibitory properties against two important alanine aminopeptidases, of human (hAPN, CD13) and porcine (pAPN) origin, were evaluated. Enzymatic studies and comparison with literature data indicated the higher inhibitory potential of the homophenylalanine over phenylalanine derivatives towards both enzymes. Their inhibition constants were in the submicromolar range for hAPN and the micromolar range for pAPN, with 1-amino-3-(3-fluorophenyl) propylphosphonic acid (compound 15c) being one of the best low-molecular inhibitors of both enzymes. To the best of our knowledge, P1 homophenylalanine analogues are the most active inhibitors of the APN among phosphonic and phosphinic derivatives described in the literature. Therefore, they constitute interesting building blocks for the further design of chemically more complex inhibitors. Based on molecular modeling simulations and SAR (structure-activity relationship) analysis, the optimal architecture of enzyme-inhibitor complexes for hAPN and pAPN were determined.
Highly diastereoselective synthesis of tetralin-fused spirooxindoles via lewis acid-catalyzed C(sp3)H bond functionalization
Machida, Mizuki,Mori, Keiji
, p. 868 - 871 (2018/07/03)
A highly diastereoselective synthesis of tetralin-fused spirooxindole derivatives was described. Treatment of benzylidene oxindoles with a catalytic amount of Sc(OTf)3 in refluxing hexane afforded the target compounds in good chemical yields with excellent diastereoselectivities (up to >20:1). Detailed investigation of the reaction mechanism revealed that both interconversion of the two diastereomers and their solubility difference in reaction medium were the key to achieving excellent diastereoselectivities.
Substitution-Controlled Selective Formation of Hexahydrobenz[ e]isoindoles and 3-Benzazepines via In(OTf)3-Catalyzed Tandem Annulations
Xing, Siyang,Gu, Nan,Wang, Xin,Liu, Jingyi,Xing, Chunyan,Wang, Kui,Zhu, Bolin
supporting information, p. 5680 - 5683 (2018/09/25)
A dramatic N-substituent controlled tandem annulation of 2-(2-(2-bromoethyl)phenyl)-1-sulfonylaziridines with 1,3-dicarbonyl compounds has been developed. When the N-substituent was a 4-methylbenzenesulfonyl group (Ts), sequential ring opening of aziridin
TRICYCLIC COMPOUNDS, PREPARATION METHODS, AND THEIR USES
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Page/Page column 85, (2012/04/10)
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
Hydrolytically-Resistant Boron-Containing Therapeutics And Methods Of Use
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Page/Page column 60, (2008/06/13)
Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
Compounds for the Treatment of Periodontal Disease
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Page/Page column 62, (2008/06/13)
Compounds, compositions and methods are provided which are useful in the treatment of periodontal disease.
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), for the potential treatment of onychomycosis
Baker, Stephen J.,Zhang, Yong-Kang,Akama, Tsutomu,Lau, Agnes,Zhou, Huchen,Hernandez, Vincent,Mao, Weimin,Alley,Sanders, Virginia,Plattner, Jacob J.
, p. 4447 - 4450 (2007/10/03)
A structure-activity relationship investigation for a more efficacious therapy to treat onychomycosis, a fungal infection of the toe and fingernails, led to the discovery of a boron-containing small molecule, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), which is currently in clinical trials for onychomycosis topical treatment.
ALPHA-(ARYL-OR HETEROARYL-METHYL)-BETA-PIPERIDINOPROPANOIC ACID COMPOUNDS AS ORL1-RECEPTOR ANTAGONISTS
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Page/Page column 32-33, (2010/11/25)
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester or salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 represents aryl or the like; -X-Y- represents
ALPHA-(ARYL-OR HETEROARYL-METHYL)-BETA PIPERIDINO PROPANAMIDE COMPOUNDS AS ORL1-RECEPTOR ANTAGONISTS
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Page/Page column 39, (2010/11/25)
This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 and R4 independently represents hydrogen or the like; R5 represents aryl or the like; -X-Y- represents -CH2O- or the like; and n represents 0, 1 or 2.These compounds have ORL1 -receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
