19261-37-1Relevant academic research and scientific papers
Enantioselective Synthesis of anti-syn-Trihalides and anti-syn-anti-Tetrahalides via Asymmetric β-Elimination
Tan, Yu,Luo, Shilong,Li, Dongmei,Zhang, Nan,Jia, Shiqi,Liu, Yidong,Qin, Wenling,Song, Choong Eui,Yan, Hailong
, p. 6431 - 6436 (2017)
Structural motifs containing contiguous halide-bearing stereocenters are common in natural products as well as bioactive molecules. A few successful examples have been reported in the area of asymmetric vicinal dihalogenation of alkenes for accessing diha
Carbene-Catalyzed Direct Functionalization of the β-sp3-Carbon Atoms of α-Chloroaldehydes
Liu, Bin,Luo, Guoyong,Wang, Hongling,Hao, Lin,Yang, Song,Jin, Zhichao,Chi, Yonggui Robin
, p. 12719 - 12723 (2019)
A direct functionalization of the β-sp3 carbon atom of α-chloro aldehyde has been developed. The reaction starts with the addition of a carbene catalyst to α-chloroaldehyde to eventually form the homoenolate intermediate. This overall redox-neu
Synthesis and anticancer properties of n-(5-r-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides
Chaban, T. I.,Matiichuk, Y. E.,Matiychuk, V. S.,Ogurtsov, V. V.,Ostapiuk, Y. V.
, p. 75 - 84 (2020/06/01)
Aim. Study of the synthesis and anticancer activity of a series of N-(5-R-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides. Methods. Organic synthesis, analytical and spectral methods, pharmacological screening. Results. N-(5-R-benzyl-1,3-thiazol-2-yl)-2
COMPOUNDS AND USES THEREOF
-
Page/Page column 322; 323, (2020/10/20)
The present invention features compounds useful in the treatment of neurological disorders and primary brain cancer. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders and primary brain cancer.
Carbene-Catalyzed α-Carbon Amination of Chloroaldehydes for Enantioselective Access to Dihydroquinoxaline Derivatives
Huang, Ruoyan,Chen, Xingkuan,Mou, Chengli,Luo, Guoyong,Li, Yongjia,Li, Xiangyang,Xue, Wei,Jin, Zhichao,Chi, Yonggui Robin
supporting information, p. 4340 - 4344 (2019/06/14)
An NHC-catalyzed α-carbon amination of chloroaldehydes was developed. Cyclohexadiene-1,2-diimines are used as amination reagents and four-atom synthons. Our reaction affords optically enriched dihydroquinoxalines that are core structures in natural products and synthetic bioactive molecules.
Synthesis of trans-2-Substituted Cyclopropylamines from α-Chloroaldehydes
West, Michael S.,Mills, L. Reginald,McDonald, Tyler R.,Lee, Jessica B.,Ensan, Deeba,Rousseaux, Sophie A. L.
supporting information, p. 8409 - 8413 (2019/10/14)
Cyclopropylamines are prevalent in pharmaceuticals and agrochemicals. Herein, we report the synthesis of trans-2-substituted cyclopropylamines in high diastereoselectivity from readily available α-chloroaldehydes. The reaction proceeds via trapping of an electrophilic zinc homoenolate with an amine followed by ring closure to generate the cyclopropylamine. We have also observed that cyclopropylamine cis/trans-isomerization occurs in the presence of zinc halide salts and that this process can be turned off by the addition of a polar aprotic cosolvent.
A general, enantioselective synthesis of 2-substituted thiomorpholines and thiomorpholine 1,1-dioxides
Reed, Carson W.,Lindsley, Craig W.
supporting information, (2019/09/10)
In the course of our drug discovery programs, we had need to access chiral, 2-substituted thiomorpholines and their oxidized congeners, thiomorpholine 1,1-dioxides. Here, we disclose a high-yielding, general protocol for the enantioselective synthesis of
Proapoptotic effects of novel thiazole derivative on human glioma cells
Finiuk, Nataliya,Klyuchivska, Olha,Ivasechko, Iryna,Hreniukh, Volodymyr,Ostapiuk, Yuriy,Shalai, Yaryna,Panchuk, Rostyslav,Matiychuk, Vasyl,Obushak, Mykola,Stoika, Rostyslav,Babsky, Andriy
, p. 27 - 37 (2019/01/03)
The aim of the present study was to investigate the antiproliferative and proapoptotic actions of N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide derivative (compound 5) in glioma cells in comparison with the actions of temozolomide
COMPOUNDS AND USES THEREOF
-
Page/Page column 315-316, (2019/10/15)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
N-Heterocyclic Carbene-Catalyzed Synthesis of α-Trifluoromethyl Esters
Gelat, Fabien,Patra, Atanu,Pannecoucke, Xavier,Biju, Akkattu T.,Poisson, Thomas,Besset, Tatiana
supporting information, p. 3897 - 3901 (2018/07/22)
The N-heterocyclic carbene (NHC)-catalyzed trifluoromethylation of α-chloro aldehydes was developed, allowing straightforward access to valuable α-trifluoromethyl ester derivatives. The unique combination of an electrophilic trifluoromethylation reagent with NHC catalysis was the key for the functionalization of a broad range of α-chloro aldehydes, and the products are formed in moderate to good yields. Investigations of the enantioselective version of this reaction afforded the enantioenriched products in moderate yields with good ee values.
