Catalytic Asymmetric Construction of a 1,2,4-Benzotriazepine Skeleton via Diastereo- and Enantioselective Decarboxylative [4 + 3] Cyclization.
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DOI: 10.1021/acs.orglett.1c00073
Abstract: We have developed a protocol for palladium-catalyzed decarboxylative [4 + 3] cycloaddition reactions between 4-vinyl benzoxazinanones and azomethine imines to generate moderate to good yields of structurally diverse 1,2,4-benzotriazepines bearing two stereogenic centers with good… read more here.
Keywords: asymmetric construction; skeleton; construction benzotriazepine; benzotriazepine skeleton ... See more keywords
Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor.
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DOI: 10.1021/acs.orglett.8b01316
Abstract: A catalytic asymmetric [3 + 2] cyclization of novel 4-isothiocyanato pyrazolones and isatin-derived ketimines was developed, delivering a wide range of intriguing dispirotriheterocyclic products in high yield with excellent diastereoselectivity and enantioselectivity. A chiral sulfoxide… read more here.
Keywords: construction multi; asymmetric construction; carboxylesterase inhibitor; human carboxylesterase ... See more keywords
Asymmetric construction of dihydrobenzofuran-2,5-dione derivatives via desymmetrization of p-quinols with azlactones.
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DOI: 10.1039/c8cc08985j
Abstract: The desymmetrization of p-quinols through a chiral bisguanidinium hemisalt catalyzed enantioselective Michael addition/lactonization cascade reaction with azlactones was reported. 3-Amino-benzofuran-2,5-diones containing a chiral amino acid residue were achieved with up to 99% ee and >19 : 1… read more here.
Keywords: construction dihydrobenzofuran; dihydrobenzofuran dione; desymmetrization quinols; asymmetric construction ... See more keywords
Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds for drug discovery.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc05700j
Abstract: Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds were achieved by intramolecular Diels-Alder reaction of bicyclic precursors derived from L-tyrosine. Three substituents were systematically introduced into the developed scaffolds in various combinations, demonstrating their high… read more here.
Keywords: construction densely; functionalized three; asymmetric construction; dimensional aza ... See more keywords