6431-73-8Relevant articles and documents
Synthesis of Chiral 2-Substituted 1,4-Benzoxazin-3-ones via Iridium-Catalyzed Enantioselective Hydrogenation of Benzoxazinones
Nie, Yu,Li, Jing,Yan, Jun,Yuan, Qianjia,Zhang, Wanbin
supporting information, p. 5373 - 5377 (2021/07/26)
An efficient iridium-catalyzed enantioselective hydrogenation of 2-alkylidene 1,4-benzoxazin-3-ones using our developed iPr-BiphPHOX as a ligand is reported. This method showed good functional group compatibility and delivered the corresponding reduced products in excellent yields (up to 99%) with excellent enantioselectivities (up to 99% ee). The reaction proceeded very well on a gram scale with low catalyst loadings (0.1 mol %), providing the product with no erosion in enantioselectivity. Additionally, three bioactive molecules can be easily obtained from the reduced products.
gSK - 3 beta inhibitor or its salt and its pharmaceutical use
-
, (2020/02/10)
The invention belongs to the pharmaceutical chemistry field, and discloses a compound for inhibiting glycogen synthase kinase-3beta (GSK-3beta) in a formula I, its pharmaceutically acceptable salt, or an application of its pharmaceutical composition for preventing and treating the GSK-3beta-related diseases. The compound is a GSK-3beta small-molecule inhibitor, its action mode is non-ATP-competitive competition, and can be used for preparing the medicines for preventing and treating the GSK-3beta-related diseases, and the GSK-3beta-related diseases can be diabetes, Alzheimer's disease, stomach cancer, colorectal cancer, pancreas cancer, liver cancer or mixed acute leukemia. According to the compound, R1, R2, R3, X, Y are consistent with detailed description in the invention.
Copper-catalyzed cascade syntheses of 2 H -benzo[ b ][1,4]thiazin-3(4 H)-ones and quinoxalin-2(1 H)-ones through capturing S and N atom respectively from AcSH and TsNH2
Chen, Dingben,Wang, Zhi-Jing,Bao, Weiliang
supporting information; experimental part, p. 5768 - 5771 (2010/10/03)
A copper-catalyzed cascade method has been developed to synthesize the 2H-benzo[b][1,4]thiazin-3(4H)-ones from 2-halo-N-(2-halophenyl)-acetamides 1 and AcSH via the SN2/deacetylation/coupling process, and to synthesize the quinoxalin-2(1H)-ones from 1 and TsNH2 via the S N2/coupling/desulfonation process. The target products were obtained with diversity at three positions on their scaffolds.
Michael additions on 2H-1,4-benzothiazin-3-ones
Chande,Suryanarayan
, p. 1094 - 1098 (2007/10/03)
Michael addition on 2H-1,4-benzothiazin-3-ones is studied in this communication. An approach towards the regioselective synthesis of Michael adducts is shown.
An Improved Alkylation of 2H-1,4-Benzothiazin-3(4H)-one and Related Heterocyclic Anilides
Marfat, Anthony,Carta, Michael P.
, p. 515 - 517 (2007/10/02)
Various N-substituted derivatives of 2H-1,4-benzothiazin-3(4H)-one are obtained in high yields employing functionalized alkyl halides and potassium tert-butoxide in dimethylformamide.The method is mild, regioselective and tolerates a variety of functional groups.