19006-81-6Relevant articles and documents
Magnesiate-Utilized/Benzyne-Mediated Approach to Indenopyridones from 2-Pyridones: An Attempt to Synthesize the Indenopyridine Core of Haouamine
Idzik, Tomasz J.,Borzyszkowska-Ledwig, Aleksandra,Struk, ?ukasz,So?nicki, Jacek G.
supporting information, p. 9667 - 9671 (2019/11/29)
An efficient, short-staged synthesis of cis-fused indeno[2,1-b]- and indeno[1,2-c]pyridin-2-ones, starting from 2-pyridones, using magnesiates of type R3MgLi as nucleophilic and deprotonation agents, mediated by benzyne generated in situ, under optimized conditions, is described. Following the developed protocol, rare C4a-arylsubstituted indeno[2,1-b]pyridones, resembling the core of haouamine, were obtained. The protocol offering the one-pot synthesis directly from 2-pyridone is also described.
ORGANIC COMPOUNDS
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Page/Page column 17, (2009/07/03)
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
8-AZABICYCLO[3.2.1]OCTANE DERIVATIVES USEFUL AS MONOAMINE REUPTAKE INHIBITORS
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Page/Page column 20, (2010/11/27)
The present invention relates to a 8-azabicyclo[3.2.1]octane derivative of Formula I, wherein R1 is H or C1-5alkyl; Y is O, S or O(CH2)m; m is 1 or 2; n is 0 or 1; Ar1 is phenylene or pyridylene, said phenylene and pyridylene being 1,3-linked with respect to O and when n is 1 with Y and when n is 0 with Ar2, said phenylene or pyridylene being optionally substituted with one or two substituents independently selected from halogen, C1-5alkyl, C1-5alkoxy, C3-6cycloalkyl, C2-5alkenyl, C2-5alkynyl, phenyl, CN and hydroxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein the oxygen of said hydroxy is optionally bonded to Ar2 to form a 5-membered ring; Ar2 is phenyl or a 5-6 membered heteroaryl, said phenyl or 5-6 membered heteroaryl being optionally substituted with one to three substituents independently selected from halogen, C1-5alkyl, C1-5alkoxy, CN, CONR2R3, CO2R4, NHCOR5 and hydroxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein the oxygen of said hydroxy is optionally bonded to Ar1 to form a 5-membered ring; R2-R4 are independently H or C1-5alkyl and R5 is C1-5alkyl, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising a 8- azabicyclo[3.2.1]octane derivative according to the present invention in admixture with one or more pharmaceutically acceptable auxiliaries and to the use of a 8- azabicyclo[3.2.1]octane derivative according to the present invention in therapy.