[EN] NOVEL 6,7-DIHYDROBENZO[A]QUINOLIZIN-2-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION<br/>[FR] NOUVEAUX DÉRIVÉS DE 6,7-DIHYDROBENZO[A]QUINOLIZIN-2-ONE POUR LE TRAITEMENT ET LA PROPHYLAXIE D'UNE INFECTION PAR LE VIRUS DE L'HÉPATITE B
申请人:HOFFMANN LA ROCHE
公开号:WO2016071215A1
公开(公告)日:2016-05-12
The invention provides novel compounds having the general formula (I) wherein R1 to R6, W and X are as described herein and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
We have succeeded in developing direct syntheses of trans β-azidohydrins and trans 1,2-diol derivatives from olefins catalyzed by dichlorotin oxide. The regioselectivity of these reactions with tri-substituted olefins is high (10:1 in the synthesis of 1,2-diol derivatives) to excellent (>99:1 in the synthesis of azidohydrins). It has been found that these reactions do not proceed via epoxides.
Novel 6,7-dihydrobenzo[a]quinolizin-2-one derivatives for the treatment and prophylaxis of hepatitis B virus infection
申请人:HOFFMANN-LA ROCHE INC.
公开号:US20160122344A1
公开(公告)日:2016-05-05
The invention provides novel compounds having the general formula:
wherein R
1
to R
6
, W and X are as described herein and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
Functionalized 3-hydroxymaleic anhydrides were prepared by cyclization of 1, 1-bis(trimethylsilyloxy)ketene acetals with oxalyl chloride. (c) 2007 Elsevier Ltd. All rights reserved.