INDUSTRIAL PROCESS FOR PREPARATION OF 1,2-DIHYDROQUINOLINE DERIVATIVE OR A SALT THEREOF, AND INTERMEDIATE FOR PREPARATION THEREOF
申请人:SANTEN PHARMACEUTICAL CO., LTD.
公开号:US20140371459A1
公开(公告)日:2014-12-18
Provided is a method for producing a compound represented by formula (7) or a salt thereof:
the method comprising the steps of:
removing a R
1
group and a R
2
group from a compound represented by formula (5) or a salt thereof:
and
reacting the compound (in which R1 and R2 in formula (5) are hydrogen atoms) obtained in the removing step or a salt thereof with a compound represented by formula (d):
or a salt thereof in the presence of a base. The method is a method for producing a 1,2-dihydroquinoline derivative having glucocorticoid receptor binding activity or a salt thereof. This method does not require a purification step by column chromatography and is suitable for industrial production.
Shi, Min; Okamoto, Yoshiki; Takamuku, Setsuo, Journal of Chemical Research, Miniprint, 1990, # 5, p. 1044 - 1054
作者:Shi, Min、Okamoto, Yoshiki、Takamuku, Setsuo
DOI:——
日期:——
Shi, Min; Okamoto, Yoshiki; Takamuku, Setsuo, Journal of Chemical Research, Miniprint, 1991, # 7, p. 1831 - 1840
作者:Shi, Min、Okamoto, Yoshiki、Takamuku, Setsuo
DOI:——
日期:——
Mechanistic Investigation of Oxygen Rebound in a Mononuclear Nonheme Iron Complex
作者:Thomas M. Pangia、Vishal Yadav、Emilie F. Gérard、Yen-Ting Lin、Sam P. de Visser、Guy N. L. Jameson、David P. Goldberg
DOI:10.1021/acs.inorgchem.9b01208
日期:2019.8.5
An iron(III) methoxide complex reacts with para-substituted triarylmethyl radicals to give iron(II) and methoxyether products. Second-order rate constants for the radical derivatives were obtained. Hammett and Marcus plots suggest the radical transfer reactions proceed via a concerted process. Calculations support the concerted nature of these reactions involving a single transition state with no initial charge transfer. These findings have implications for the radical "rebound" step invoked in nonheme iron oxygenases, halogenases, and related synthetic catalysts.
HUSZTHY, P.;LEMPERT, K.;SIMIG, G.;TAMAS, J., J. CHEM. SOC. PERKIN TTRANS., 1982, N 12, 1671-1674