62306-79-0Relevant articles and documents
Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors
Zheng, Hongbo,Li, Lin,Sun, Bin,Gao, Yun,Song, Wei,Zhao, Xiaoyu,Gao, Yanhui,Xie, Zhiyu,Zhang, Nianzhao,Ji, Jianbo,Yuan, Huiqing,Lou, Hongxiang
supporting information, p. 30 - 38 (2018/03/08)
Based on perlolyrine (1), a natural alkaloid with weak PDE5 potency from the traditional Chinese aphrodisiac plant Tribulus terrestris L., a series α-substituted tetrahydro-β-carboline (THβC) derivatives were synthesized via T+BF4--mediated oxidative C–H functionalization of N-aryl THβCs with diverse potassium trifluoroborates. Following Winterfeldt oxidation afforded the corresponding furyl/thienyl pyrroloquinolones, of which 5-ethylthiophene/ethylfuran derivatives 20a–b were identified as the most potent and selective PDE5 inhibitors. Among the enantiomers, (S)-20a and (S)-20b (IC50 = 0.52 and 0.39 nM) were found to be more effective than their (R)-antipode, display favorable pharmacokinetic profiles, exert in vitro vasorelaxant effects on the isolated thoracic aorta, and exhibit in vivo efficacy in the anesthetized rabbit erectile model.
Metallocene complex and olefin polymerization method (by machine translation)
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Paragraph 0139, (2017/05/16)
PROBLEM TO BE SOLVED: To provide a metallocene complex that incorporates ethylene and an α-olefin as comonomers with better efficiency than conventional metallocene catalysts and gives a polymerized high-molecular weight rubber component in copolymerization of olefins including propylene as a monomer, and produces homopolypropylene having a high melting point in homopolymerization of propylene, and to provide an olefin polymerization method using the same.SOLUTION: The metallocene catalyst is represented by general formula [I], which has a cyclic structure between the 5- and 6-positions of the indenyl ring and has an optionally substituted furyl or thienyl group at the 2-position of the indenyl ring. The olefin polymerization catalyst comprises the metallocene complex. The olefin polymerization method comprises polymerizing or copolymerizing olefins by using the olefin polymerization catalyst.
METALLOCENE COMPOUND AND METHOD OF PRODUCING OLEFIN POLYMER WITH POLYMERIZATION CATALYST USING THE SAME
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Paragraph 0103, (2017/01/02)
PROBLEM TO BE SOLVED: To provide: a catalyst that can produce a high molecular weight rubber component and enables efficient production of a block copolymer having a high ethylene or α-olefin content with a desired content ratio in the rubber part; and a method of producing an olefin polymer using the same. SOLUTION: The present invention provides a metallocene complex represented by the general formula [I]. COPYRIGHT: (C)2015,JPOandINPIT
A C-H borylation approach to suzuki-miyaura coupling of typically unstable 2-heteroaryl and polyfluorophenyl boronates
Robbins, Daniel W.,Hartwig, John F.
supporting information; experimental part, p. 4266 - 4269 (2012/10/08)
A method for the synthesis of biaryls and heterobiaryls from arenes and haloarenes without the intermediacy of unstable boronic acids is described. Pinacol boronate esters that are analogous to unstable boronic acids are formed in high yield by iridium-catalyzed C-H borylation of heteroarenes and fluoroarenes. These boronates are stable in the solid state or in solution and can be generated and used in situ. They couple with aryl halides in the presence of simple palladium catalysts, providing a convenient route to biaryl and heteroaryl products that have been challenging to prepare via boronic acids.
TRIAZOLO [4, 5-D] PYRAMIDINE DERIVATIVES AND THEIR USE AS PURINE RECEPTOR ANTAGONISTS
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Page/Page column 29, (2010/01/30)
Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
COMPOUNDS, COMPOSITIONS AND METHODS
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Figure 11, (2008/06/13)
The present invention provides methods and pharmaceutical compositions for inhibiting expressions of HIF and HIF regulated genes, inhibiting angiogenesis, inducing cell cycle arrest in tumor cells, and treating cell proliferating diseases or conditions.
Metallocene compounds, processes for the production of olefin polymers using catalysts containing the compounds, and olefin polymers produced by the processes
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Page/Page column 30-31, (2010/02/07)
Metallocene compounds represented by the following general formula (1): YqKLMX2??(1) wherein M, Y, q, L and X are each as defined in the Specification.
