2732-90-3Relevant articles and documents
Radical C(sp3)-H Heck-type Reaction of N-Alkoxybenzimidoyl Chlorides with Styrenes to Construct Alkenols
Fang, Di,Zhang, Yidan,Chen, Yiyun
supporting information, p. 2050 - 2054 (2022/03/17)
We report the first radical C(sp3)-H Heck-type reaction of aliphatic alcohols for selective δ- and ?-alkenol synthesis by photoredox catalysis. N-Alkoxybenzimidoyl chlorides are developed as novel alkoxyl radical precursors with tunable redox potentials. Various alkenols can be constructed by the inert C(sp3)-H Heck-type reaction of 4-cyano-N-alkoxybenzimidoyl chlorides with styrene derivatives under redox-neutral conditions, which can be performed on the gram scale and can be easily derivatized.
Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis
Chen, Lin-Hai,Fang, You-Chen,Nan, Fa-Jun,Xiao, Yu-Feng,Xie, Xin,Zhang, Qing
supporting information, p. 3991 - 4006 (2022/03/14)
GPR84 is a proinflammatory G protein-coupled receptor associated with several inflammatory and fibrotic diseases. GPR84 antagonists have been evaluated in clinical trials to treat ulcerative colitis, idiopathic pulmonary fibrosis, and nonalcoholic steatohepatitis. However, the variety of potent and selective GPR84 antagonists is still limited. Through high-throughput screening, a novel phosphodiester compound hit 1 was identified as a GPR84 antagonist. The subsequent structural optimization led to the identification of compound 33 with improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. In a DSS-induced mouse model of ulcerative colitis, compound 33 significantly alleviated colitis symptoms and reduced the disease activity index score at oral doses of 25 mg/kg qd, with an efficacy similar to that of positive control 5-aminosalicylic acid (200 mg/kg, qd, po), suggesting that compound 33 is a promising candidate for further drug development.
Synthesis of Trifluoromethylated Tetrasubstituted Allenes via Palladium-Catalyzed Carbene Transfer Reaction
Koenigs, Rene M.,Pei, Chao,Yang, Zhen
supporting information, p. 7300 - 7304 (2020/10/02)
Herein, we report on the palladium-catalyzed synthesis of trifluoromethylated, tetrasubstituted allenes from vinyl bromides and trifluoromethylated diazoalkanes in good to excellent yield. This reaction proceeds via oxidative addition of a Pd(0) complex w
Intermolecular Radical C(sp3)?H Amination under Iodine Catalysis
Bosnidou, Alexandra E.,Mu?iz, Kilian
supporting information, p. 7485 - 7489 (2019/04/30)
The direct amination of aliphatic C?H bonds has remained one of the most tantalizing transformations in organic chemistry. Herein, we report on a unique catalyst system, which enables the elusive intermolecular C(sp3)?H amination. This practical synthetic strategy provides access to aminated building blocks and fosters innovative multiple C?H amination within a new approach to aminated heterocycles. The synthetic utility is demonstrated by the synthesis of four relevant pharmaceuticals.
Radical C?H Bond Trifluoromethylation of Alkenes by High-Valent Copper(III) Trifluoromethyl Compounds
Zhang, Hao-Ran,Xiao, Chang,Zhang, Song-Lin,Zhang, Xiaoming
supporting information, p. 5305 - 5310 (2019/11/22)
A general and selective method is developed that allows direct vinylic C?H bond trifluoromethylation of 1,1-diarylalkenes by a high-valent copper(III) trifluoromethyl complex, producing biologically active trifluoromethylated alkenes (as well as trifluoro
IRIDIUM (III) COMPLEXES WITH CYCLIC QUINOXALINE-FUSED LIGANDS AND ORGANIC LIGHT-EMITTING DIODES USING THE SAME
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, (2018/11/26)
An iridium (III) complex compound with cyclic quinoxaline-fused dibenzosuberene ligand is shown in General Formula (1), wherein m is 1 or 2, n is 1 or 2, and m+n is 3; A is a bridging atom represented by General Formula (2) or General Formula (3), wherein R1 is a hydrogen atom, alkyl or tert-butyl group, R2 to R14 are independently selected from the group consisting of hydrogen atom, halogen atom, cyano group, alkyl group, cycloalkyl group, aryl group, alkoxy group, amino group, thioalkyl group, silyl group and alkenyl group.
Iridium complex of cyclic quinoxaline condensed ligand and organic light-emitting diode component
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, (2018/12/02)
The invention provides iridium complex of a cyclic quinoxaline condensed ligand and an organic light-emitting diode component. The structure of the complex is as shown in general formula (1), whereinm is 1 or 2, n is 1 or 2, and m+n=3; A is an bridging atom with a structure as shown in general formula (2) or general formula (3), R1 is a hydrogen atom, alkyl or a tert-butyl group, and R1-R14 are selected from one of independent hydrogen atom, halogen atom, cyano group, alkyl, aryl, naphthenic group, alkoxy, amino, haloalkane group, sulfane group, silane group and alkenyl group.
IRIDIUM (III) COMPLEXES WITH CYCLIC QUINOXALINE-FUSED LIGANDS AND ORGANIC LIGHT-EMITTING DIODES USING THE SAME
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, (2019/05/15)
An iridium (III) complex compound with cyclic quinoxaline-fused dibenzosuberene ligand is shown in formula (1),wherein m is 1 or 2, n is 1 or 2, and m + n is 3 A is a bridging atom represented by formula (2) or formula (3), wherein R1 is a hydrogen atom, alkyl group or tert-butyl group, R2 to R14 are independently selected from the group consisting of hydrogen atom, halogen atom, cyano group, alkyl group, cycloalkyl group, aryl group, alkoxy group, amino group, thioalkyl group, silyl group and alkenyl group.
Construction of dibenzo-fused seven- to nine-membered carbocycles via Bronsted acid-promoted intramolecular Friedel - Crafts-type alkenylation
Otani, Takashi,Ueki, Kanako,Cho, Kinryo,Kanai, Kan,Tateno, Kotaro,Saito, Takao
, p. 7895 - 7898 (2015/05/13)
Bronsted acid-promoted intramolecular hydroarylation of alkynylbenzenes carrying an arylalkyl group at the ortho-position leads to alkylidenedibenzo[a,d]cycloheptenes, -octenes and -nonenes in up to quantitative yield with complete regioselectivity. The scope and limitation of this reaction and application to the synthesis of tricyclic antidepressants are described.
TRICYCLIC STEROID HORMONE NUCLEAR RECEPTOR MODULATORS
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Page 220, (2008/06/13)
The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).
