METHOD FOR PRODUCING PYRAZOLE FUSED RING DERIVATIVE
申请人:Eisai R&D Management Co., Ltd.
公开号:EP2202233A1
公开(公告)日:2010-06-30
Disclosed is a commercially advantageous method for producing a pyrazole fused ring derivative (such as a 7-phenylpyrazolo[1,5-a]pyridine derivative). Specifically disclosed is a method for producing a compound (I) represented by the formula (I) below or a salt thereof, which comprises a step A wherein a hydroxy group in a compound (IV) represented by the formula (IV) below is converted into a methoxy group, thereby obtaining a compound (I) or a salt thereof:
Intermolecular C–H Amidation of Alkenes with Carbon Monoxide and Azides via Tandem Palladium Catalysis
作者:Zheng-Yang Gu、Yang Wu、Xiaoguang Bao、Ji-Bao Xia、Feng Jin
DOI:10.1055/a-1401-4486
日期:2021.9
alkenes with carbonmonoxide and organic azides has been developed for the synthesis of alkenyl amides. The reaction proceeds efficiently without an ortho-directing group on the alkene substrates. Nontoxic dinitrogen is generated as the sole by-product. Computational studies and control experiments have revealed that the reaction takes place via an unexpected mechanism by tandem palladium catalysis.
intramolecular aglycon delivery (IAD), whereby a glycosyl acceptor is temporarily appended to a hydroxyl group of a glycosyl donor is an attractive method that can allow the synthesis of 1,2-cis glycosides in an entirely stereoselective fashion. 2-O-Allyl protected thioglycoside donors are excellent substrates for IAD, and may be glycosylated stereoselectively through a three-step reaction sequence. This sequence
Asymmetric Radical Process for General Synthesis of Chiral Heteroaryl Cyclopropanes
作者:Xiaoxu Wang、Jing Ke、Yiling Zhu、Arghya Deb、Yijie Xu、X. Peter Zhang
DOI:10.1021/jacs.1c04655
日期:2021.7.28
applicable to α-pyridyl and other α-heteroaryldiazomethanes for asymmetriccyclopropanation of wide-ranging alkenes, including several types of challenging substrates. This new catalytic methodology provides a general access to valuable chiral heteroaryl cyclopropanes in high yields with excellent both diastereoselectivities and enantioselectivities. Combined computational and experimental studies further
Nazarov Cyclizations of an Allenyl Vinyl Ketone with Interception of the Oxyallyl Cation Intermediate for the Formation of Carbon−Carbon Bonds
作者:Vanessa M. Marx、D. Jean Burnell
DOI:10.1021/ja909073r
日期:2010.2.10
substitution on the diene. Cyclic dienes react with the oxyallyl cation by forming only one carbon-carbon bond, but the site of bond formation can be affected by steric hindrance. Electron-rich alkenes intercept the allyl cation by forming one carbon-carbon bond, or two carbon-carbonbonds through [3 + 2] cyclization. In some instances, further treatment of the initial products with BF(3) x Et(2)O leads