- Synthesis of 2-Substituted Quinolines via Rhodium(III)-Catalyzed C–H Activation of Imidamides and Coupling with Cyclopropanols
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An efficient synthesis of 2-substituted quinolines from readily available cyclopropanols and imidamides has been developed, where the cyclopropanol acts as a C3 synthon. With the assistance of a bifunctional imidamide directing group, the reaction occurred via sequential C–H/C–C cleavage and C–C/C–N bond formation. (Figure presented.).
- Zhou, Xukai,Qi, Zisong,Yu, Songjie,Kong, Lingheng,Li, Yang,Tian, Wan-Fa,Li, Xingwei
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- Rare-Earth Y(OTf)3 Catalyzed Coupling Reaction of Ethers with Azaarenes
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Rare-earth catalysis has become a hot topic in the field of catalytic organic reaction. Chain ethers mostly have lower reactivity and lower boiling points which limited their reaction scope. Herein, we found a rare-earth Y(OTf)3 can catalyze th
- Wu, Yue-Hua,Wang, Nai-Xing,Zhang, Tong,Zhang, Lei-Yang,Gao, Xue-Wang,Xu, Bao-Cai,Xing, Yalan,Chi, Jian-Yi
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- Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships
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This series of reports describes the development of orally active, highly potent, specific antagonists of the peptidoleukotrienes containing a (2-quinolinylmethoxy)phenyl moiety. Described in this first report are the structure-activity relationships that led to more than a 20-fold improvement of the potency and selectivity of the initial chemical lead (RG 5901). From this series of compounds, RG 7152 (16) was identified and selected for further evaluation in the clinic as an antiasthmatic agent. Compound 16 competitively inhibits [3H]LTD4 binding to membranes from guinea pigs lung (K(i) = 38 ± 6 nM) and the spasmogenic activity of LTC4, LTD4, and LTE4 in parenchymal lung strips from guinea pigs. Unlike the original lead (RG 5901), compound 16 does not inhibit 5-lipoxygenase from guinea pig PMNs. Following oral administration to guinea pigs, 16 blocks LTD4-induced dermal permeability (ED50 = 6.9 mg/kg), LTD4-induced bronchoconstriction (ED50 = 1.1 mg/kg), antigen-induced bronchoconstriction (ED50 = 2.5 mg/kg), and anaphylactic-induced mortality (ED50 = 16 mg/kg). These studies on structure-activity relationships indicate that there is a requirement for an acidic function and the presence of the (2-quinolinylmethoxy)phenyl moiety in a specific geometric arrangement.
- Youssefyeh,Magnien,Lee,Chan,Lin,Galemmo Jr.,Johnson Jr.,Tan,Campbell,Huang,Nuss,Carnathan,Sutherland,Van Inwegen
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p. 1186 - 1194
(2007/10/02)
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- Aryl and heteroaryl ethers as agents for the treatment of hypersensitive ailments
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The present invention is concerned with the therapeutic composition comprising as an active ingredient a compound of the formula: and salts thereof; wherein Ar and Ar1 are independently phenyl, naphthyl or a nitrogen, oxygen, or sul
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