- Nickel-Catalyzed C-O Bond-Cleaving Alkylation of Esters: Direct Replacement of the Ester Moiety by Functionalized Alkyl Chains
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Two efficient protocols for the nickel-catalyzed aryl-alkyl cross-coupling reactions using esters as coupling components have been established. The methods enable the selective oxidative addition of nickel to acyl C-O and aryl C-O bonds and allow the aryl-alkyl cross-coupling via decarbonylative bond cleavage or through cleavage of a C-O bond with high efficiency and good functional group compatibility. The protocols allow the streamlined, unconventional utilization of widespread ester groups and their precursors, carboxylic acids and phenols, in synthetic organic chemistry.
- Liu, Xiangqian,Jia, Jiaqi,Rueping, Magnus
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p. 4491 - 4496
(2017/07/24)
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- A Novel Series of Selective, Non-Peptide Inhibitors of Angiotensin II Binding to the AT2 Site
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The availability of peptide and non-peptide Ang II receptor antagonists has permitted the study of Ang II receptor heterogeneity.It is now widely recognized that there are at least two distinct Ang II receptor subtypes.AT1 receptors are selective in their recognition of agents such as losartan, DuP 532,L-158,809,SKF108566, and similar non-peptides.To date, all of the well-known actions of Ang II in mammals are blocked by the AT1 selective antagonists such as losartan and are thus designated as being mediated by the AT1 receptor.Although there have been reports of functional activity mediated through AT2 sites, the pharmacological role for the AT2 receptor has not yet been elucidated.Herein, we report the chemistry and SAR on a novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids which have selective affinity for AT2 receptors.The most potent of which (19) has an IC50 of 30 nM for the AT2 receptor in the rat adrenal radioligand binding assay.
- VanAtten, Mary K.,Ensinger, Carol L.,Chiu, Andrew T.,McCall, Dale E.,Nguyen, Tam T.,et al.
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p. 3985 - 3992
(2007/10/02)
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- New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships
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(p-Amylcinnamoyl)anthranilic acid (3a) had moderate antagonist activities against LTD4-induced smooth muscle contraction on guinea pig ileum and LTC4-induced bronchoconstriction in anesthetized guinea pigs. Modifications were made in the hydrophobic part (cinnamoyl moiety) and the hydrophilic part (anthranilate moiety) of 3a. A series of 8-(benzoylamino)-2-tetrazol-5-yl-1,4-benzodioxans and 8-(benzoylamino)-2-tetrazol-5-yl-4-oxo-4H-1-benzopyrans were revealed to be potent antagonists of leukotrienes C4 and D4. Among both series, ONO-RS-347 (18k) and ONO-RS411 (19h) were the most potent and orally active antagonists, respectively. Structure-activity relationships are discussed.
- Nakai,Konno,Kosuge,Sakuyama,Toda,Arai,Obata,Katsube,Miyamoto,Okegawa,Kawasaki
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