Method for producing benzylidene derivatives

作者: Nobuhiro Haga , Susumu Kamata , Masanao Inagaki , Saichi Matsumoto

DOI:

关键词: Base (group theory)Medicinal chemistryRing (chemistry)AlkylHalogenStereochemistryAlkoxy groupPhenyleneArylChemistry

摘要: The present invention is directed to a selective method for producing given stereoisomeric benzylidene derivatives of the formula III: wherein R1 and R2 each independently lower alkyl, alkoxy or halogen; Y SO2, SO CO; -A- optionally substituted alkylene; -B- -CH2- -O-; taken together may form phenylene alkenylene; R hydrogen, cycloalkyl, alkoxy, hydroxy, aryl, arylalkyl; arylalkyloxy, heterocyclic ring N-protecting groups, which comprises reacting compound I: are as defined above X halogen with II: Y, -A-, in presence base. compounds useful non-steroidal anti-inflammatory agents.

参考文章(5)
Nobuhiro Nankonaka Chome Haga, Susumu Hikarigaoka Chome Kamata, Takeshi D Shiota, Saichi Fushiodai Chome Matsumoto, Toshihiko Minamitawaracho Okada, Hirokuni Horennarayamacho Jyoyama, 3-benzylidene-1-carbamoyl-2-pyrrolidone analogues ,(1992)
S. Wong, S. J. Lee, M. R. Frierson, J. Proch, T. A. Miskowski, B. S. Rigby, S. J. Schmolka, R. W. Naismith, D. C. Kreutzer, R. Lindquist, Antiarthritic profile of BF-389--a novel anti-inflammatory agent with low ulcerogenic liability. Inflammation Research. ,vol. 37, pp. 90- 98 ,(1992) , 10.1007/BF01987895
Charles M. Orlando, Quinone methide chemistry. Benzylic oxidative methoxylation of 2,6-di-tert-butyl-p-cresol Journal of Organic Chemistry. ,vol. 35, pp. 3714- 3717 ,(1970) , 10.1021/JO00836A028
Eiichi Ohsugi, Toshiro Konoike, Toru Chisan Mansion Ichijoji Kita, Hiroshi Harada, 2,4,6-substituted phenol derivatives ,(1990)