[EN] COMPOUNDS FOR TREATING CNS DISORDERS<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE TROUBLES DU SYSTÈME NERVEUX CENTRAL
申请人:SAGE THERAPEUTICS INC
公开号:WO2020264512A1
公开(公告)日:2020-12-30
Provided herein in part is a compound of Formula (I): or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of using the compounds, e.g, in the treatment of CNS- related disorders.
Selectivity in the cycloadditions of carbonyl ylides with glyoxylates: an approach to the zaragozic acids—squalestatins
作者:David M. Hodgson、James M. Bailey、Carolina Villalonga-Barber、Michael G. B. Drew、Timothy Harrison
DOI:10.1039/b004870o
日期:——
Reaction of diazodiketoester 8 with glyoxylates in the presence of catalytic rhodium(II) acetate generates 6,8-dioxabicyclo[3.2.1]octanes 9 and 11 in good yield. Elaboration of 9 provides a suitable alcohol 25 for acid-catalysed rearrangement to give the 2,8-dioxabicyclo[3.2.1]octane skeleton 26 of the zaragozic acidsâsqualestatins. More substituted diazodiketoesters 36 and 40 also undergo highly regio- and diastereoselective cycloaddition with glyoxylates to give the cycloadducts 41, 43 and 44.
A mild, efficient method for the oxidation of α-diazo-β-hydroxyesters to α-diazo-β-ketoesters
作者:Puhui Li、Max M. Majireck、Ilia Korboukh、Steven M. Weinreb
DOI:10.1016/j.tetlet.2008.03.011
日期:2008.5
alpha-diazo-beta-ketoesters can be prepared in good overall yields via a two-step sequence involving addition of ethyl lithiodiazoacetate to aliphatic, aromatic and conjugated aldehydes followed by mildoxidation with the Dess-Martin periodinane.
Metallkatalysierte zersetzung von 4-diazomethyl-4H-pyranen - ein neuer zugang in das oxepinsystem
作者:Karl-Ludwig Hoffmann、Manfred Regitz
DOI:10.1016/s0040-4039(00)87867-3
日期:——
Electrophilic diazoalkane substitution of lithiated diazomethyl compounds (5) with the pyrylium salt 4 leads to the formation of the hitherto unknown 4-diazomethyl 4H-pyranes 6. Their decomposition with catalytic amounts of μ-allyl palladium chloride (dimer) in benzene is followed by ring enlargement to the oxepines 8, which are not in equilibrium with the valence tautomeric benzene oxides 7.
Various 4- and 4,5-substituted 2,7-di-tert-butylthiepins such as 4-ethoxycarbonyl-(6), 4-formyl- (7), 4-hydroxymethyl- (8), 4-methyl- (12), 4-methy1-5-hydroxymethy1-(13), and 4,5-dimethyl derivatives (16), and so on, were synthesized by functional group transformation and some of their properties were examined.