110013-19-9Relevant academic research and scientific papers
Discovery of phenylpyrrolidine derivatives as a novel class of retinol binding protein 4 (RBP4) reducers
Akao, Yuichiro,Cho, Nobuo,Furuyama, Naoki,Goto, Akihiko,Kamaura, Masahiro,Kasai, Shizuo,Mizukami, Atsushi,Nakamura, Natsuko,Nakamura, Shinji
supporting information, (2021/12/30)
Retinol-binding protein 4 (RBP4) is a potential drug target for metabolic and ophthalmologic diseases. A high-throughput screening of our compound library has identified a small-molecule RBP4 reducer 7a, as a hit compound. Aiming to provide a suitable too
Preparation method of chiral 3-substituted pyrrolidine derivative
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Paragraph 0068-0069, (2020/11/01)
The invention provides a preparation method of a chiral 3-substituted pyrrolidine derivative. The preparation method comprises an intermediate preparation step, a diastereomer mixture preparation step, a chiral separation step and a chiral 3-substituted pyrrolidine derivative synthesis step. According to the invention, through catalytic asymmetric kinetic resolution, a mixture of two diastereoisomers is efficiently converted into a diastereoisomer with a certain single configuration, chiral separation is realized, a key intermediate is obtained with high yield, and a series of chiral 3-substituted pyrrolidine derivatives are synthesized. The whole reaction route is mild in reaction condition, simple and convenient to operate, high in resolution efficiency, high in atom economy, low in costand suitable for industrial scale production.
Method for synthesizing N-Boc-3-pyrrolidine formaldehyde
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Paragraph 0032; 0034; 0039; 0042; 0044, (2017/06/02)
The invention discloses a method for synthesizing N-Boc-3-pyrrolidine formaldehyde. The method comprises that dimethyl itaconate as a raw material undergoes an intramolecular cyclization reaction to produce methyl 5-oxo-3-pyrrolidine carboxylate, then the methyl 5-oxo-3-pyrrolidine carboxylate undergoes a reduction reaction to produce pyrrolidine-3-methanol, then the pyrrolidine-3-methanol is subjected to Boc protection so that N-Boc-pyrrolidine-3-methanol is obtained, and finally, the N-Boc-pyrrolidine-3-methanol is oxidized to form a final product compound. The method is simple and convenient, has a low cost, content greater than 99%, produces small environmental pollution and is suitable for industrial production.
TRICYCLIC COMPOUNDS FOR USE IN THE TREATMENT AND/OR CONTROL OF OBESITY
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Paragraph 00588-00590, (2014/05/24)
The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against me
Concise synthesis of bicyclic aminals by way of catalytic intramolecular C-H amination and evaluation of their reactivity as iminium precursors
Rodriguez-Lucena, David,Morin, Marie S.T.,Compain, Philippe
scheme or table, p. 155 - 162 (2012/04/04)
The concise synthesis of fused bicyclic aminals by way of intramolecular rhodium-catalyzed C-H amination is reported as well as the evaluation of their reactivity as iminium precursors. In contrast to the well-studied N,O-acetal systems, the aminals synthesized were found to be particularly stable under reaction conditions used for nucleophilic addition.
PYRIMIDONE DERIVATIVES USED AS TAU PROTEIN KINASE 1 INHIBITORS
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, (2011/02/24)
A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C-X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1 -C3 alkyl group; L represents single bond or a C1 -C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
AURORA KINASE COMPOUNDS AND METHODS OF THEIR USE
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Page/Page column 186, (2011/08/04)
Provided herein are pyrrolotriazine compounds for treatment of Aurora kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
Iron(III)-catalyzed consecutive aza-cope-mannich cyclization: Synthesis of trans -3,5-dialkyl pyrrolidines and 3,5-dialkyl-2,5-dihydro-1 H-pyrroles
Carballo, Ruben M.,Purino, Martin,Ramirez, Miguel A.,Martin, Victor S.,Padron, Juan I.
supporting information; experimental part, p. 5334 - 5337 (2011/01/05)
An efficient alkene aza-Cope-Mannich cyclization between 2-hydroxy homoallyl tosylamine and aldehydes in the presence of iron(III) salts to obtain 3-alkyl-1-tosyl pyrrolidines in good yields is described. The process is based on the consecutive generation of a γ-unsaturated iminium ion, 2-azonia-[3,3]-sigmatropic rearrangement, and further intramolecular Mannich reaction. Iron(III) salts are also shown to be excellent catalysts for the new aza-Cope-Mannich cyclization using 2-hydroxy homopropargyl tosylamine.
Disubstituted pyrimidines as Lck inhibitors
Hunt, Julianne A.,Beresis, Richard T.,Goulet, Joung L.,Holmes, Mark A.,Hong, Xinfang J.,Kovacs, Ernest,Mills, Sander G.,Ruzek, Rowena D.,Wong, Frederick,Hermes, Jeffrey D.,Park, Young-Whan,Salowe, Scott P.,Sonatore, Lisa M.,Wu, Lin,Woods, Andrea,Zaller, Dennis M.,Sinclair, Peter J.
supporting information; experimental part, p. 5440 - 5443 (2010/04/26)
We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cell
Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the α6* subtype
Breining, Scott R.,Bencherif, Merouane,Grady, Sharon R.,Whiteaker, Paul,Marks, Michael J.,Wageman, Charles R.,Lester, Henry A.,Yohannes, Daniel
scheme or table, p. 4359 - 4363 (2010/04/05)
Direct comparison of pyridine versus pyrimidine substituents on a small but diverse set of ligands indicates that the pyrimidine substitution has the potential to enhance affinity and/or functional activity at α6 subunit-containing neuronal nicotinic rece
