5-Ring Heteroaromatic compounds and their use as binding partners for 5-ht5 receptors
申请人:Amberg Wilhelm
公开号:US20110207788A1
公开(公告)日:2011-08-25
The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.
这项发明涉及一般式(I)的5-环杂芳化合物,其用于治疗和/或预防疾病,以及含有这些化合物的药物。
Indium(i) iodide-catalyzed regio- and diastereoselective formal α-addition of an α-methylallylboronate to N-acylhydrazones
作者:Shū Kobayashi、Hideyuki Konishi、Uwe Schneider
DOI:10.1039/b802153h
日期:——
Indium(I) iodide was found to catalyze the formal α-addition of an α-methylallylboronate to various N-acylhydrazones, in the presence of an alcohol additive, to afford the corresponding anti-α-adducts with high regio- and diastereoselectivity in high yields.
Aza-Michael Addition Reactions of Hydrazones with Activated Alkynes Catalyzed by Nitrogen-Containing Organic Bases
作者:Zhi-Liang Yuan、Yin Wei、Min Shi
DOI:10.1002/ejoc.201000365
日期:2010.7
2]-octane)-catalyzed Michael-type reactions of hydrazones with activatedalkynes are described in this paper. This aza-Michaeladditionreaction can be applied to different types of hydrazones, such as hydrazones 1 and hydroxy-bearing hydrazones 5. The corresponding adducts are achieved in high yields under mild reaction conditions. DABCO-promoted aza-Michaeladditionreactions were successfully applied to
Cyanation of N-acylhydrazones using trimethylsilylcyanide (TMSCN) proceeded well in the presence of an amine to afford the corresponding α-hydrazinonitriles in high yields. For less reactive substrates, the combined use of an amine and a catalytic amount of scandium triflate [Sc(OTf)3] was effective to promote the reactions. The mechanistic study suggested that the amine worked as a Brønstedbase
Trifluoromethylation of <i>N</i>-Benzoylhydrazones
作者:Alexander D. Dilman、Dmitry E. Arkhipov、Vitalij V. Levin、Pavel A. Belyakov、Alexander A. Korlyukov、Marina I. Struchkova、Vladimir A. Tartakovsky
DOI:10.1021/jo800782w
日期:2008.7.1
A method for the nucleophilic trifluoromethylation of N-benzoylhydrazones using Me3SiCF3/AcONa has been described. The C=N bond of the hydrazones is activated by difluoroboron group, which is introduced by means of boron trifluoride and allylsilane.