Solid phase synthesis of 1,5-disubstituted pyrazole-4-hydroxamic acids and pyrazole-4-carboxamides via direct amidation of β-ketoesters
作者:Weixu Zhai、Samuel W. Gerritz、Michael J. Sofia
DOI:10.1016/j.tetlet.2011.11.031
日期:2012.1
This manuscript describes a convenient method for the directamidation of methyl and ethyl β-ketoesters to generate solid-supported β-ketohydroxamates or β-ketoamides and the application of this methodology to the synthesis of 1,5-disubstituted pyrazole-4-hydroxamic acids and pyrazole-4-carboxamides.
[EN] CARBOLINE AND BETACARBOLINE DERIVATIVES FOR USE AS HDAC ENZYME INHIBITORS<br/>[FR] DERIVES DE CARBOLINE ET DE BETACARBOLINE INHIBITEURS DE L'ENZYME HDAC
申请人:CHROMA THERAPEUTICS LTD
公开号:WO2004113336A1
公开(公告)日:2004-12-29
Compounds of formula (IA) and (IB) are inhibitors of histone deacetylase activity and useful for the treatment of, inter alia, cancers: wherein fused rings A1 and A2 are optionally substituted; linker radical R1 represents a radical of formula
Method for Activation and Recycling of Trityl Resins
作者:Itedale Namro Redwan、Morten Grøtli
DOI:10.1021/jo300598d
日期:2012.8.17
anilines onto a polystyrene triphenylmethyl (trityl) resin. High loadings were obtained in a matter of minutes by treating resin-bound trityl chloride with triethyloxonium tetrafluoroborate followed by alcohols or anilines. Yields were comparable or better than known literature methods. Recycling of the recovered resin was also possible using the developed method.
Substituted hexahydropyrazino (1,2-a) pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments
申请人:Flohr Stefanie
公开号:US20050004131A1
公开(公告)日:2005-01-06
Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.
Compounds of the formula I
in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.