- Lewis acid-promoted site-selective cyanation of phenols
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An efficient Lewis acid-promoted site-selective electrophilic cyanation of 3-substituted and 3,4-disubstituted phenols has been developed. The cyanation reactions using MeSCN as the cyanating reagent proceeded efficiently to afford a wide range of 2-hydroxybenzonitriles with high efficiency and excellent regioselectivity. This protocol could provide a practical method for the synthesis and modification of biologically active molecules.
- Yang, Wen,Zhang, Wu,Zhao, Wanxiang
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supporting information
p. 4604 - 4609
(2020/07/04)
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- Nonspecific medium effects versus specific group positioning in the antibody and albumin catalysis of the base-promoted ring-opening reactions of benzisoxazoles
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The mechanisms by which solvents, antibodies, and albumins influence the rates of base-catalyzed reactions of benzisoxazoles have been explored theoretically. New experimental data on substituent effects and rates of reactions in several solvents, in an antibody, and in an albumin are reported. Quantum mechanical calculations were carried out for the reactions in water and acetonitrile, and docking of the transition state into a homology model of antibody 34E4 and an X-ray structure of human serum albumin was accomplished. A microenvironment made up of catalytic polar groups (glutamate in antibody 34E4 and lysine in human serum albumin) surrounded by relatively nonpolar groups is present in both catalytic proteins.
- Hu, Yunfeng,Houk,Kikuchi, Kazuya,Hotta, Kinya,Hilvert, Donald
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p. 8197 - 8205
(2007/10/03)
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- Studies on agents with vasodilator and β-blocking activities. V. Synthesis and pharmacological activity of the optical isomers of TZC-5665
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Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among the four optical isomers, R(A),S(B)-one (1c) possessed the essential activities of TZC-5665 (1).
- Seki, Toshimi,Kanada, Arihiro,Nakao, Tomio,Shiraiwa, Masahumi,Asano, Hajime,Miyazawa, Katuhiko,Ishimori, Tsutomu,Minami, Nobuyoshi,Shibata, Kenyu,Yasuda, Kikuo
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