633294-91-4Relevant articles and documents
MACROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE
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, (2020/07/14)
The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
Remote stereocontrol in the Nazarov reaction: A new approach to the core of roseophilin
Occhiato, Ernesto G.,Prandi, Cristina,Ferrali, Alessandro,Guarna, Antonio
, p. 4542 - 4545 (2007/10/03)
Three different procedures are compared to obtain properly substituted divinyl ketones in which one of the double bonds is embedded in a five-membered heterocyclic structure and therefore suitable to produce cyclopenta-fused pyrrole derivatives by the acid-catalyzed Nazarov reaction. These, on treatment with TFA, afforded 2,4-cis-disubstituted 2,3,4,5-tetrahydro-1H-cyclopenta[e] pyrrol-6-ones with high stereo-control. One of these Nazarov products was oxidized to the corresponding 4,5-dihydro-1H-cyclopenta[e]pyrrol-6-one derivative, thus obtaining an enantiopure key intermediate in the total synthesis of roseophilin.