- Regio- and Stereoselective Synthesis of Benzo-δ-sultams by Palladium-Catalyzed Hydrocarbonation of Alkynes
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An efficient method for the synthesis of benzo-δ-sultams [(4Z)-4-benzylidene-2-(arylmethyl)-3,4-dihydro-2H-1,2-benzothiazine 1,1-dioxides] via palladium(0)-catalyzed hydrocarbonation of alkynes is presented. This method allows regioselective access to a variety of substituted benzosultams in excellent yields under mild conditions. The stereochemistry of the exocyclic double bond of the benzosultam derivatives is confirmed by single-crystal X-ray diffraction.
- Debnath, Sudarshan,Mondal, Shovan
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p. 710 - 722
(2016/03/01)
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- FLAP MODULATORS
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The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention
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Paragraph 0249
(2015/11/03)
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- Lewis acid catalyzed cascade reaction of 3-(2-benzenesulfonamide)propargylic alcohols to spiro[indene-benzosultam]s
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A highly efficient and convenient construction of the spiro[indene-benzosultam] skeleton from propargylic alcohols has been developed. The reaction proceeded in a Lewis acid catalyzed cascade process, including the trapping of allene carbocation with sulfonamide, electrophilic cyclization, and intramolecular Friedel-Crafts alkylation. In the presence of NIS or NBS, iodo/bromo-substituted spiro[indene-benzosultam]s could be prepared in excellent yields.
- Sun, Lang,Zhu, Yuanxun,Wang, Jing,Lu, Ping,Wang, Yanguang
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supporting information
p. 242 - 245
(2015/02/19)
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- Construction of nitrogen heterocycles bearing an aminomethyl group by copper-catalyzed domino three-component coupling-cyclization
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(Chemical Equation Presented) A direct approach to 2-(aminomethyl)indoles by copper-catalyzed domino three-component coupling-cyclization of 2-ethynylanilines with a secondary amine and aldehyde has been developed. By use of a cyclic or acyclic secondary
- Ohta, Yusuke,Chiba, Hiroaki,Oishi, Shinya,Fujii, Nobutaka,Ohno, Hiroaki
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supporting information; experimental part
p. 7052 - 7058
(2009/12/06)
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- Regioselective construction of six-membered fused heterocyclic rings via Pd/C-mediated C-C coupling followed by iodocyclization strategy: a new entry to 2H-1,2-benzothiazine-1,1-dioxides
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We describe a practical and elegant method of constructing a thiazine ring fused with benzene under mild reaction conditions. A?variety of 4-iodo-2H-benzo[e][1,2]thiazine-1,1-dioxides were prepared with high regioselectivity via a two-step process involvi
- Barange, Deepak Kumar,Batchu, Venkateswara Rao,Gorja, Dhillirao,Pattabiraman, Vijaya Raghavan,Tatini, Lakshmi Kumar,Babu, J. Moses,Pal, Manojit
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p. 1775 - 1789
(2007/10/03)
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- AMINOQUINAZOLINES COMPOUNDS
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The present invention is concerned with compounds of formula (1), wherein R1, R2 and X are as defined in the description and claims. The compounds of the present invention are PTP-1B inhibitors and can be used as medicaments.
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Page/Page column 91
(2008/06/13)
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