[EN] MODULATORS OF THE GLUCOCORTICOID RECEPTOR<br/>[FR] MODULATEURS DU RECEPTEUR GLUCOCORTICOIDE
申请人:PFIZER PROD INC
公开号:WO2004005229A1
公开(公告)日:2004-01-15
The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1-R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor ágonist.therapy. Glucocorticoid-receptor modulators are useful in the treatment of certain inflammatory conditions.
Homolytic aromatic substitutions of pentatomic heteroaromatics with electrophilic carbon radicals generated by alkyl halides and triethylborane
作者:Enrico Baciocchi、Ester Muraglia
DOI:10.1016/s0040-4039(00)74072-x
日期:1993.7
An efficient homolytic aromatic substitution of pyroles, furan and thiophene by ·CH2CO2Et and ·CH(CH3)CO2Et has been carried out, the radicals being generated by autoxidation of BEt3 in the presence of XCH2CO2Et and XCH(CH3)CO2Et (X=Br, I).
已经进行了·CH 2 CO 2 Et和·CH(CH 3)CO 2 Et对吡咯,呋喃和噻吩的有效均质芳族取代,自由基是在XCH 2 CO 2存在下通过BEt 3的自氧化产生的。Et和XCH(CH 3)CO 2 Et(X = Br,I)。
Modulators of the glucocorticoid receptor
申请人:Pfizer Inc.
公开号:US20040138262A1
公开(公告)日:2004-07-15
The present invention provides compounds of the formula
1
wherein A is of the formula
2
and X, Y, n, R
1
-R
25
are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
The present invention provides compounds of the formula
wherein A is of the formula
and X, Y, n, R
1
—R
25
are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
Homolytic substitution reactions of electron-rich pentatomic heteroaromatics by electrophilic carbon-centered radicals. Synthesis of .alpha.-heteroarylacetic acids
Efficient and selective homolytic substitutions (yields between 55 and 90%) of pyrrole, indole, and some pyrrole derivatives have been carried out using ambiphilic and electrophilic carbon centered radicals, generated in DMSO by Fe2+/H2O2 and alpha-cyano-, alpha-carbonyl-, and alpha,alpha'-dicarbonylalkyl iodides. The reaction is highly successful also with pyrroles substituted by electron-withdrawing groups, which has allowed an efficient synthesis of Tolmetin. A few extensions of this reaction to furan and thiophene are described.