1766-57-0Relevant articles and documents
Palladium-catalyzed intramolecular oxidative coupling involving double C(sp2)-H bonds for the synthesis of annulated biaryl sultams
Laha, Joydev K.,Jethava, Krupal P.,Dayal, Neetu
, p. 8010 - 8019 (2014)
The palladium-catalyzed intramolecular oxidative coupling described herein involves a double C(sp2)-H bond functionalization in sulfonanilides, providing a workable access to biaryl sultams annulated into a six-membered ring that are otherwise difficult to obtain by literature methods. The other synthetic applications of this protocol including the synthesis of biaryl sultams containing a seven-membered ring and analogous sultones are also presented.
INHIBITORS OF RAC1 AND USES THEREOF FOR INDUCING BRONCHODILATATION
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Paragraph 0072; 0073, (2019/01/04)
The present invention concerns a compound having the following formula (I): wherein: - A is in particular -N(R'a)-C(=O)-R, R'a being H or a (C1-C6)alkyl group, and R being preferably a group having the following formula (II): - X is in particular chosen from the group consisting of: -SO2-N(R'b)-, R'b being H or a (C1-C6)alkyl group, -N(R"b)-SO2-, R"b being H or a (C1-C6)alkyl group, -CO-NH-, and -NH-CO-, for use for the treatment of pathologies characterized by bronchoconstriction, such as asthma.
Highly specific N-monomethylation of primary aromatic amines
Le Pera, Adolfo,Leggio, Antonella,Liguori, Angelo
, p. 6100 - 6106 (2007/10/03)
A synthetic methodology for the specific conversion of primary aromatic amines into their N-monomethyl derivatives under very mild conditions is presented. Anilines are treated with 4-nitrobenzenesulfonyl (nosyl) chloride to generate the corresponding sulfonamides 2 in high yields. The subsequent N-methylation reaction of the sulfonamides 2 with a solution of diazomethane is rapid and quantitative. Removal of the nosyl protecting group is readily carried out using the reagent system mercaptoacetic acid/1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) affording the N-monomethylated aromatic amines 4. The procedure is convenient, efficient, and gives rise to the N-monomethyl-anilines exclusively.