Corey-Chaykovsky Cyclopropanation of Nitronaphthalenes: Access to Benzonorcaradienes and Related Systems
Nitronaphthalene derivatives react as Michael acceptors in the Corey-Chaykovsky reaction with alkyl phenyl selenones and alkyl diphenyl sulfonium salts. Mechanistic studies reveal that sterically demanding substituents at the carbanionic center favor formation of cyclopropanes and suppress competitive β-elimination to the alkylated products. The transformation, demonstrated also on heterocyclic nitroquinoline and nitroindazolines, is an example of transition metal-free dearomatization method.
Antoniak, Damian,Barbasiewicz, Micha?
supporting information
p. 9320 - 9325
(2019/11/19)
TRIAZOLO PYRIDINES AS MODULATORS OF GAMMA-SECRETASE
The present invention relates to triazolo pyridines of formula (II) and their use as modulators of ?-secretase. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the form
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Page/Page column 15
(2019/07/13)
Discovery of tetrahydroindazoles as a novel class of potent and in vivo efficacious gamma secretase modulators
The identification and optimization of a novel series of centrally efficacious gamma secretase modulators (GSMs) offering an alternative to the privileged aryl imidazole motif is described. Chiral bicyclic tetrahydroindazolyl amine substituted triazolopyr
An expedient, regioselective synthesis of novel 2-alkylamino- and 2-alkylthiothiazolo[5,4-e]- and -[4,5-g]indazoles and their anticancer potential
Several novel 2-alkylamino- and 2-alkylthiothiazolo[5,4-e]- and -[4,5-g]indazoles and their 6-alkyl and 8-alkyl derivatives have been synthesised in high overall yields starting from 5-nitro and 6-nitroindazoles in a three-step route involving the regioselective cyclisation of thioureidoindazoles and indazolyl dithiocarbamates as the key steps. Some assorted thiazoloindazoles have been screened for anticancer properties, which demonstrated the anticancer potential of at least one product, justifying its further follow-up.
Efficient and regioselective synthesis of 2-alkyl-2H-indazoles
An efficient and regioselective synthesis of 2-methyl-2H-indazoles and 2-ethyl-2H-indazoles using trimethyloxonium tetrafluoroborate or triethyloxonium hexafluorophosphate is reported.
Cheung, Mui,Boloor, Amogh,Stafford, Jeffrey A.
p. 4093 - 4095
(2007/10/03)
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