Manganese(III)-mediated carbon-carbon bond formation in the reaction of xanthenes with active methylene compounds
摘要:
Oxidation of xanthenes with manganese(III) acetate in the presence of active methylene compounds such as 1,3-dicarbonyl compounds, malononitrile derivatives, acetone, and nitromethane selectively gives 9-substituted xanthene derivatives in good yields. A similar oxidation of thioxanthene also yields 2-(9-thioxanthenyl)-1,3-dicarbonyl compounds in 57-91% yields. The obtained 2-(9-xanthenyl)-1,3-dicarbonyl compounds are readily converted to 2-(9-xanthenylidene)-1,3-dicarbonyl derivatives using manganese(III) complexes or 2,3-dichloro-5, 6-dicyano-1,4-benzoquinone. The mechanisms for the formation of 9-substituted xanthenes are discussed on the basis of the reaction of intermediates, the electron-donating substituent effect on the xanthene ring system, effect of additives, and comparison with a reaction of radical-trapping reagents.
[EN] COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES<br/>[FR] COMPOSÉS POUR TRAITER DES MALADIES NEURODÉGÉNÉRATIVES
申请人:ARRAY BIOPHARMA INC
公开号:WO2011123674A1
公开(公告)日:2011-10-06
The invention provides novel spirotetrahydronaphthalene compounds of Formula α that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
[EN] HETEROCYCLIC INHIBITORS OF BETA - SECRETASE FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES<br/>[FR] INHIBITEURS HÉTÉROCYCLIQUES DE LA BÊTA-SECRÉTASE POUR LE TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
申请人:ARRAY BIOPHARMA INC
公开号:WO2012071458A1
公开(公告)日:2012-05-31
The invention provides novel tricyclic compounds of Formula I' that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
[EN] PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII<br/>[FR] MACROCYCLES PEPTIDIQUES CONTRE ACINETOBACTER BAUMANNII
申请人:HOFFMANN LA ROCHE
公开号:WO2017072062A1
公开(公告)日:2017-05-04
The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
[EN] SPIROINDOLINONES AS DDR1 INHIBITORS<br/>[FR] SPIROINDOLINONES UTILISÉS EN TANT QU'INHIBITEURS DE DDR1
申请人:HOFFMANN LA ROCHE
公开号:WO2017137334A1
公开(公告)日:2017-08-17
The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
2-Acylaminopropanamines as growth hormone secretagogues
申请人:ELI LILLY AND COMPANY
公开号:EP0761219A1
公开(公告)日:1997-03-12
This invention provides a series of substituted propanamines which are useful in treating a physiological condition which may be modulated by an increase in growth hormone. This invention also provides methods for the treatment of such physiological conditions which comprise administering a growth hormone secretagogue as described in the present invention in combination with growth hormone releasing hormone.