29619-31-6Relevant academic research and scientific papers
Preparation method of sulfonyl amidine with 2-Picolylamine and DMF-DMA as amine sources
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Paragraph 0080; 0082, (2020/09/09)
The invention discloses a preparation method of sulfonyl amidine with 2-Picolylamine and DMF-DMA as amine sources. The method comprises the following steps: reacting sulfonyl chloride with 2-Picolylamine to obtain an intermediate product; and then reacting the intermediate product with DMF-DMA in the presence of a catalyst at a temperature of 60-100 DEG C, then performing cooling to room temperature, extracting the reaction solution with ethyl acetate, performing layering, drying and then concentrating to obtain a target product sulfonyl amidine. According to the method disclosed by the invention, the reaction of secondary sulfonamide and DMF-DMA is realized, and the synthesis path of sulfonyl amidine is expanded. The synthetic reaction is simple in operation, mild in condition and convenient in post-treatment, and the obtained intermediate product and the product are high in purity and yield.
SUBSTITUTED BICYCLIC HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
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Page/Page column 45, (2018/05/24)
The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
SUBSTITUTED 6-MEMBERED ARYL OR HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
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Page/Page column 36, (2018/05/24)
The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
N -Sulfonyl acetylketenimine as a highly reactive intermediate for the synthesis of N -sulfonyl amidines
Yang, Weiguang,Huang, Dayun,Zeng, Xiaobao,Luo, Dongping,Wang, Xinyan,Hu, Yuefei
supporting information, p. 8222 - 8225 (2018/07/29)
A highly reactive intermediate N-sulfonyl acetylketenimine was generated from a 3-butyn-2-one participating CuAAC/ring-opening method. Its high reactivity due to bearing two EWGs allowed us to offer the first example of a reaction between ketenimine and amide to synthesize N-sulfonyl amidines efficiently.
ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
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Paragraph 0505, (2017/10/13)
The present disclosure relates to compounds of formula I that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation
4-Substituted-2,3,5,6-tetrafluorobenzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, XII, and XIII
Dudutiene, Virginija,Zubriene, Asta,Smirnov, Alexey,Gylyte, Joana,Timm, David,Manakova, Elena,Gra?ulis, Saulius,Matulis, Daumantas
, p. 2093 - 2106 (2013/04/24)
A series of 4-substituted-2,3,5,6-tetrafluorobenezenesulfonamides were synthesized and their binding potencies as inhibitors of recombinant human carbonic anhydrase isozymes I, II, VII, XII, and XIII were determined by the thermal shift assay, isothermal
Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
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Page/Page column 57, (2009/09/07)
This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R′, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.
Topically active carbonic anhydrase inhibitors. 4. [(hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides
Shepard,Graham,Hudcosky,Michelson,Scholz,Schwam,Smith,Sondey,Strohmaier,Smith,Sugrue
, p. 3098 - 3105 (2007/10/02)
For several decades a tantalizing goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase inhibitor. Recent results from several research groups indicate that considerable progress has been made toward this objective. In this report, we present the design and synthesis of (hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides. These compounds exhibit inhibition of carbonic anhydrase II in the nanomolar range and lower intraocular pressure in the α-chymotrypsinized rabbit model of ocular hypertension after topical instillation.
