177748-63-9Relevant articles and documents
Intramolecular Anti-Carbolithiation of Alkynes: Stereo-Directing Effect of Lithium-Coordinating Substituents
Ly, Kim Uyen,Boussonnière, Anne,Castanet, Anne-Sophie
supporting information, (2022/01/19)
This paper presents the results of our investigations on the stereochemical course of intramolecular carbolithiation of alkynes. It is shown that the presence of a lithium-chelating propargylic substituent completely reverses the otherwise favored syn-pro
Synthesis of Amides and Esters by Palladium(0)-Catalyzed Carbonylative C(sp3)?H Activation
?arny, Tomá?,Baudoin, Olivier,Clemenceau, Antonin,Rocaboy, Ronan
supporting information, p. 18980 - 18984 (2020/09/01)
The 1,4-palladium shift strategy allows the functionalization of remote C?H bonds that are difficult to reach directly. Reported here is a domino reaction proceeding by C(sp3)?H activation, 1,4-palladium shift, and amino- or alkoxycarbonylation, which generates a variety of amides and esters bearing a quaternary β-carbon atom. Mechanistic studies showed that the aminocarbonylation of the σ-alkylpalladium intermediate arising from the palladium shift is fast using PPh3 as the ligand, and leads to the amide rather than the previously reported indanone product.
2-METHYL-QUINAZOLINES
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Page/Page column 376-377, (2018/10/19)
The present invention describes 2-methyl-quinazoline compounds of general formula (I), methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions. The 2-methyl substituted quinazoline compounds of general formula(I) effectively and selectively inhibit the Ras-Sos interaction without significantly targeting the EGFR receptor. They are therefore useful for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, such as cancer as a sole agent or in combination with other active ingredients.