177748-63-9Relevant academic research and scientific papers
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
Borylation of Unactivated C(sp3)-H Bonds with Bromide as a Traceless Directing Group
Zhang, Ge,Li, Meng-Yao,Ye, Wen-Bo,He, Zhi-Tao,Feng, Chen-Guo,Lin, Guo-Qiang
supporting information, p. 2948 - 2953 (2021/05/05)
A palladium-catalyzed alkyl C-H borylation with bromide as a traceless directing group is described, providing a convenient approach to access alkyl boronates bearing a β-all-carbon quaternary stereocenter. The protocol features a broad substrate scope, excellent site selectivity, and good functional group tolerance.
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.
Highly Selective Synthesis of Tetrahydronaphthaleno[60]fullerenes via Fullerene-Cation-Mediated Intramolecular Cyclization
Yang, Xiao-Yu,Lin, Hao-Sheng,Matsuo, Yutaka
, p. 16314 - 16322 (2019/12/25)
A high-yielding protocol to construct six-membered carbon rings on fullerene is presented. This methodology with in situ fullerene-cation-mediated intramolecular cyclization provides high selectivity and efficient access to six-membered tetrahydronaphthal
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.
Chiral Magnesium Bisphosphate-Catalyzed Asymmetric Double C(sp3)-H Bond Functionalization Based on Sequential Hydride Shift/Cyclization Process
Mori, Keiji,Isogai, Ryo,Kamei, Yuto,Yamanaka, Masahiro,Akiyama, Takahiko
supporting information, p. 6203 - 6207 (2018/05/23)
Described herein is a chiral magnesium bisphosphate-catalyzed asymmetric double C(sp3)-H bond functionalization triggered by a sequential hydride shift/cyclization process. This reaction consists of stereoselective domino C(sp3)-H bond functionalization: (1) a highly enantio- and diastereoselective C(sp3)-H bond functionalization by chiral magnesium bisphosphate (first [1,5]-hydride shift), and (2) a highly diastereoselective C(sp3)-H bond functionalization by an achiral catalyst (Yb(OTf)3, second [1,5]-hydride shift).
BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENT
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, (2011/10/10)
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds are of the formula, wherein Y' is a halogen, Y is halosubstituted alkyl, or a salt thereof.
Synthesis of N-alkoxyindol-2-ones by copper-catalyzed intramolecular N-arylation of hydroxamates
Kukosha, Tatyana,Trufilkina, Nadezhda,Katkevics, Martins
supporting information; experimental part, p. 2525 - 2528 (2011/11/13)
The first example of copper-catalyzed intramolecular N-arylation of hydroxamic acid derivatives is presented. Based on this transformation a new method for the synthesis of N-alkoxyindol-2-ones from 2-(2-bromoaryl) acetylhydroxamates has been developed. T
