336628-65-0Relevant academic research and scientific papers
Silylaryl Halides Can Replace Triflates as Aryne Precursors
Mesgar, Milad,Daugulis, Olafs
, p. 3910 - 3913 (2016)
Silylaryl bromides and iodides can be prepared in one step from commercially available starting materials. Arynes can be generated from these compounds under conditions nearly identical to those employed for silylaryl triflates. Three distinct transformat
ASK1 INHIBITING AGENTS
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Page/Page column 194, (2018/09/08)
Provided are compounds of Formulas (I'), (I), (II') and (II), or pharmaceutically acceptable salts thereof, and methods for their use and production.
Synthesis of obscuraminol A using an organocatalyzed enantioselective Henry reaction
Filippova, Liudmila,Antonsen, Simen,Stenstr?m, Yngve,Hansen, Trond Vidar
supporting information, p. 6572 - 6577 (2016/09/23)
The first synthesis of the polyunsaturated amino alcohol natural product obscuraminol A is reported. This stereoselective synthesis was based on an anti- and enantioselective organocatalyzed Henry reaction followed by a chemoselective SmI2-mediated reduction that affected only the nitro-group of the Henry product. These efforts yielded obscuraminol A where the configuration of the all-Z skipped double bonds was conserved from the starting material, i.e. the ethyl ester of (all-Z)-eicosa-5,8,11,14,17-pentaenoic acid. Our synthesis confirmed the reported structure of obscuraminol A.
NOVEL PHENOL DERIVATIVE
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Page/Page column 10, (2012/07/28)
Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in FIG. 1; a pharmaceutically acceptable salt t
Highly enantioselective henry reactions in water catalyzed by a copper tertiary amine complex and applied in the synthesis of (S)-N-trans-feruloyl octopamine
Lai, Guoyin,Guo, Fengfeng,Zheng, Yueqin,Fang, Yang,Song, Haigang,Xu, Kun,Wang, Sujing,Zha, Zhenggen,Wang, Zhiyong
supporting information; scheme or table, p. 1114 - 1117 (2011/03/21)
It's in the water! A new copper tertiary amine complex was prepared and applied in asymmetric Henry reactions in water and in the short synthesis of (S)-N-trans-feruloyl octopamine. This catalytic system provided an approach to the enantioselective Henry reaction of aldehydes with hydroxyl substituents (see graphic).
TRPV1 ANTAGONISTS
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Page/Page column 62-63, (2010/04/30)
Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
TRPV1 ANTAGONISTS
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Page/Page column 61, (2010/04/30)
Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Synthesis and evaluation of novel inhibitors of pim-1 and pim-2 protein kinases
Xia, Zuping,Knaak, Christian,Jian, Ma.,Beharry, Zanna M.,McInnes, Campbell,Wang, Wenxue,Kraft, Andrew S.,Smith, Charles D.
experimental part, p. 74 - 86 (2009/09/25)
The Pim protein kinases are frequently overexpressed in prostate cancer and certain forms of leukemia and lymphoma. 5-(3-Trifluoromethylbenzylidene) thiazolidine-2,4-dione (4a) was identified by screening to be a Pim-1 inhibitor and was found to attenuate the autophosphorylation of tagged Pim-1 in intact cells. Although 4a is a competitive inhibitor with respect to ATP, a screen of approximately 50 diverse protein kinases demonstrated that it has high selectivity for Pim kinases. Computational docking of 4a to Pim-1 provided a model for lead optimization, and a series of substituted thiazolidine-2,4-dione congeners was synthesized. The most potent new compounds exhibited IC 50s of 13 nM for Pim-1 and 2.3 μM for Pim-2. Additional compounds in the series demonstrated selectivities of more than 2500-fold and 400-fold for Pim-1 or Pim- 2, respectively, while other congeners were essentially equally potent toward the two isozymes. Overall, these compounds are new Pim kinase inhibitors that may provide leads to novel anticancer agents.
Chiral zirconium catalysts using multidentate BINOL derivatives for catalytic enantioselective Mannich-type reactions; ligand optimization and approaches to elucidation of the catalyst structure
Ihori, Yoichi,Yamashita, Yasuhiro,Ishitani, Haruro,Kobayashi, Shu
, p. 15528 - 15535 (2007/10/03)
Catalytic enantioselective Mannich-type reactions of silicon enolates with aldimines were investigated using chiral zirconium catalysts prepared from Zr(OtBu)4, N-methylimidazole, and newly designed multidentate BINOL derivatives. Th
The synthesis and use in asymmetric epoxidation of metal salen complexes derived from enantiopure trans-cyclopentane- and cyclobutane-1,2-diamine
Daly, Adrian M.,Gilheany, Declan G.
, p. 127 - 137 (2007/10/03)
A complete synthesis of enantiopure trans-cyclopentane-1,2-diamine and trans-cyclobutane-1,2-diamine is described. These diamines have been used as components of novel chiral salen ligands whose chromium and manganese complexes were then evaluated as oxygen transfer agents in the asymmetric epoxidation of alkenes.
