186605-19-6Relevant academic research and scientific papers
Construction of Chiral-Fused Tricyclic γ-Lactams via a trans-Perhydroindolic Acid-Catalyzed Asymmetric Domino Reaction
An, Qianjin,Shen, Jiefeng,Liu, Delong,Liu, Yangang,Zhang, Wanbin
, p. 2925 - 2928 (2017)
An asymmetric domino reaction was developed utilizing readily available cyclic α-dehydroamino ketones and aldehydes, which when subjected a 2-iodoxybenzoic acid (IBX)-mediated oxidation gives pyrrolidinone-containing tricyclic derivatives. trans-Perhydroi
Concise synthesis and applications of enantiopure spirobiphenoxasilin-diol and its related chiral ligands
Liu, Tao,Wang, Biqin,Wang, Peng,Wu, Yichen,Xu, Wen-Qiang,Yang, Lei
supporting information, p. 13365 - 13368 (2021/12/17)
The development of chiral architectures for chiral ligand and catalyst discovery is essential for asymmetric catalysis. Herein, we report the concise synthesis of a Si-centered spirocyclic skeleton, spirobiphenoxasilin-diol (SPOSiOL), and its derived chiral ligands. Using the chemical resolution method, the optical SPOSiOL could be obtained in high yield on a gram scale. Preliminary studies indicated that this ligand scaffold has great potential in transition metal-catalyzed asymmetric reactions. This finding further highlights that the Si-centered spirocyclic scaffolds are of great value in asymmetric catalysis. This journal is
Compounds serving as BACE1 inhibitors and application thereof
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Paragraph 0218; 0220-0222, (2020/04/17)
The invention belongs to the field of medical chemistry and relates to compounds serving as BACE1 inhibitors and application of the compounds. Specifically, the invention provides the compounds as shown in a formula I which is described in the specification or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, a preparation method of the compounds, pharmaceutical compositions containing the compounds and application of the compounds or the compositions to treatment and/or prevention of BACE1 related diseases, such as Alzheimer's disease, Huntington's disease, Down's syndrome, beta-like amyloid vascular disease and the like. The compounds provided by the invention show very good inhibitory activity on hBACE1 enzyme, has lower inhibitory activity on hCathepsin D enzyme, is high in selectivity, and is very expected to become a therapeutic agent for BACE1 related diseases and with higher curative effect and smaller side effects.
Silver-Promoted Direct Phosphorylation of Bulky C(sp2)-H Bond to Build Fully Substituted β-Phosphonodehydroamino Acids
Cao, Hao-Qiang,Liu, Hao-Nan,Liu, Zhe-Yuan,Qiao, Baokun,Zhang, Fa-Guang,Ma, Jun-An
supporting information, p. 6414 - 6419 (2020/09/02)
A general and practical cross-dehydrogenative coupling protocol between readily available trisubstituted α,β-dehydro α-amino carboxylic esters and H-phosphites is described. This C(sp2)-H phosphorylation reaction proceeds with absolute Z-selectivity promoted by silver salt in a radical relay manner. The bulky tetrasubstituted β-phosphonodehydroamino acids were obtained in grams and added new modules to the toolkit for peptide modifications.
An Atropos Chiral Biphenyl Bisphosphine Ligand Bearing Only 2,2′-Substituents and Its Application in Rh-Catalyzed Asymmetric Hydrogenation
Jia, Jia,Ling, Zheng,Zhang, Zhenfeng,Tamura, Ken,Gridnev, Ilya D.,Imamoto, Tsuneo,Zhang, Wanbin
supporting information, p. 738 - 743 (2017/12/26)
An atropos chiral biphenyl bisphosphine ligand bearing only 2,2′-substituents was rationally designed and easily synthesized utilizing a bulky chiral t-butylmethylphosphino block. Computational results showed a large difference in the free energies betwee
ANTIDIABETIC ENOLIC GLUCOSIDE OF PHENYLPYRUVIC ACID
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Paragraph 0207; 0208; 0209, (2018/09/22)
PROBLEM TO BE SOLVED: To provide an antidiabetic enolic glucoside of phenylpyruvic acid and derivatives thereof, for use as medicaments, especially normoglycemic agents, i.e. for lowering blood glucose levels to normal levels in mammals that are obese, pre-diabetic or have diabetes, obesity and/or syndrome X. SOLUTION: Compounds of the present invention help to manage blood glucose levels, i.e. helping the body by balancing the blood glucose levels; helping to keep balanced blood glucose levels, particularly in humans with diabetes; aiding by enhancing the glucose uptake by the cells and by reducing blood glucose levels, thus improving or restoring the glucose tolerance; optimizing the glycemic response; and normalizing the glucose tolerance. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
An Atropos Biphenyl Bisphosphine Ligand with 2,2′-tert-Butylmethylphosphino Groups for the Rhodium-Catalyzed Asymmetric Hydrogenation of Enol Esters
Jia, Jia,Fan, Dongyang,Zhang, Jian,Zhang, Zhenfeng,Zhang, Wanbin
supporting information, p. 3793 - 3800 (2018/09/20)
This is an update of our previous work concerning the development of Atropos biphenyl bisphosphine ligands. An unexpected Atropos structural property was confirmed by single crystal X-ray diffraction and this result is consistent with the computational calculations described in our previous work. This P-stereogenic bisphosphine ligand possessing a biphenyl backbone and 2,2′-tert-butylmethylphosphino groups has been applied to the Rh-catalyzed asymmetric hydrogenation of enol esters, which has not been widely studied and can be used for the synthesis of several important bioactive compounds. Although there is room for further improvement in enantioselectivity, the results reported herein provide a further understanding of such types of ligands. (Figure presented.).
Green fluorescent protein chromophore derivatives as a new class of aldose reductase inhibitors
Saito, Ryota,Hoshi, Maiko,Kato, Akihiro,Ishikawa, Chikako,Komatsu, Toshiya
, p. 965 - 974 (2016/10/25)
A number of (Z)-4-arylmethylene-1H-imidazol-5(4H)-ones, which are related to the fluorescent chromophore of the Aequorea green fluorescent protein (GFP), have been synthesized and evaluated their in vitro inhibitory activity against recombinant human aldo
ANTIDIABETIC ENOLIC GLUCOSIDE OF PHENYLPYRUVIC ACID
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Paragraph 0207; 0208; 0209, (2016/10/07)
PROBLEM TO BE SOLVED: To provide an antidiabetic enolic glucoside of phenylpyruvic acid and derivatives thereof, for use as medicaments, especially normoglycemic agents, i.e. for lowering blood glucose levels to normal levels in mammals that are obese, pr
Methylglucoside phenylpyruvic acid Antidiabetes enolic type (by machine translation)
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Paragraph 0207; 0208; 0209, (2016/10/31)
PROBLEM TO BE SOLVED: pharmaceutical, especially sugar normal agent, in other words, for antiobestic, before the diabetes, or diabetes, Antiobesic and/or of a mammal having X syndrome sugar is lowered to a normal value to be used as a medicine, phenylpyruvic acid and its derivatives methylglucoside antidiabetes enolic type. SOLUTION: the compound of the present invention, useful for managing hypoglycaemia, in other words, by balancing hypoglycaemia physical condition; a balanced sugar, especially of human diabete balanced helps keep the blood sugar level; by sthenia gulucose taken by cells, by lowering the value of sugar helps and, hence, to improve the recovery or tolerance; optimizing a sugar response; tolerance. Selected drawing: no (by machine translation)
