60211-57-6Relevant academic research and scientific papers
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities
Martin, Stephen F.,Walby, Grant D.
supporting information, (2022/04/09)
A number of substituted norbenzomorphans have been previously identified as high affinity ligands for the two known sigma receptors σ1R and σ2R/TMEM97, and some norbenzomorphans that are selective for σ2R/TMEM97 exhibit promise in animal models of several neurological disorders. Toward further assessing the effects of simplifying the norbenzomorphan scaffold, sets of 6-membered heterocycles were designed and prepared, and their binding affinities for σ1R and σ2R/TMEM97 were determined. Consistent with our design strategy, N-acyl-2-arylpiperidines show high affinity for σ2R/TMEM97, whereas those derived from morpholine and N-methylpiperazine have lower affinities. However, most of these 6-membered heterocycles unexpectedly exhibit even higher affinity for σ1R and are thus σ1R-selective. Computational docking studies show that representative 6-membered heterocycles bind and interact with σ2R/TMEM97 in a manner similar to that of a docked structure of their norbenzomorphan parent. Collectively, these binding and computational studies support our design strategy for developing simplified analogs of norbenzomorphans as σ2R/TMEM97 ligands, but they also underscore the challenges associated with developing selective modulators of σ2R/TMEM97.
Preparation method of 3, 5-dichlorobenzaldehyde and carboxamide triazole intermediate
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Paragraph 0045, (2021/02/10)
The invention relates to a preparation method of 3, 5-dichlorobenzene methanol and a carboxylamine triazole intermediate. The preparation method of the 3, 5-dichlorobenzene methanol comprises the following steps: mixing the 3, 5-dichlorobenzene methanol with potassium borohydride and zinc chloride in a solvent, heating to reflux, and carrying out reduction reaction; after the reduction reaction isfinished, concentrating to prepare a crude product; and adding a hydrochloric acid aqueous solution and toluene into the crude product for extraction or adding toluene for extraction, collecting a toluene phase, washing the toluene phase with an alkaline aqueous solution and water to be neutral, then concentrating the toluene phase to be dry, and recrystallizing the obtained solid with n-hexane.According to the synthetic method of 3, 5-dichlorobenzene methanol, the raw materials are easy to obtain, the reaction conditions are mild and easy to control, the product is easy to purify, and the yield of the product is high.
Silica-coated Fe3O4 magnetic nanoparticles-supported sulfonic acid as a highly active and reusable catalyst in chemoselective deprotection of tert-butyldimethylsilyl (TBDMS) ethers
Hossein Javadi, Sayed,Zareyee, Daryoush,Monfared, Azam,Didehban, Khadijeh,Mirshokraee, Sayed Ahmmad
supporting information, p. 7 - 12 (2019/11/03)
Anchored propyl sulfonic acid on the surface of silica-coated magnetic nanoparticles (Fe3O4@SiO2@PrSO3H) was successfully employed in the deprotection of TBDMS ethers. The prepared magnetically separable nanocatalyst exhibited efficient catalytic activity with high conversion and selectivity in cleavage of TBDMS ethers. TBDMS ethers are efficiently cleaved to the corresponding hydroxyl compounds in methanol solution containing 2 mol% magnetic nano-catalysts. Good to excellent yields of products, simple work-up and product separation, selective cleavage of TBDMS ethers in the presence of TBDPS ethers, easy recycling of the catalyst with external magnet with no loss in its activity (7 reaction cycles) are important features of this new protocol.
N-(Substituted sulfonyl)benzamide derivative and preparation method and pharmaceutical application thereof
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Paragraph 0329; 0331-0335, (2019/04/17)
The invention relates to an N-(substituted sulfonyl)benzamide derivative and preparation method and pharmaceutical application thereof, in particular to an N-(substituted sulfonyl)benzamide derivativeshown as general formula (I), preparation method thereof, medicinal salts of the derivative, and their application as therapeutics, especially as Nav1.7 inhibitors, wherein substituents in the general formula (I) shown in the description are defined the same as in the description.
AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS
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, (2008/06/13)
There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
Binding activity of substituted benzyl derivatives of chloronicotinyl insecticides to housefly-head membranes, and its relationship to insecticidal activity against the housefly Musca domestica
Nishiwaki, Hisashi,Nakagawa, Yoshiaki,Takeda, David Y.,Okazawa, Atsushi,Akamatsu, Miki,Miyagawa, Hisashi,Ueno, Tamio,Nishimura, Keiichiro
, p. 875 - 881 (2007/10/03)
Variously substituted benzyl derivatives of chloronlcotinyl insecticides were synthesized with a wide range of substituents including halogens, NO2, CN, CF3 and small alkyl and alkoxy groups at the ortho, meta and para positions, as well as multiple-substituted benzyl analogues. Their binding activity to the α-bungarotoxin binding site in housefly (Musca domestica) head membrane preparations was measured. Among the compounds tested, the activity of the meta-CN derivative was the highest, being 20-100 times higher than those of imidacloprid, acetamiprid and nitenpyram. The synergized insecticidal activity against houseflies was also measured for selected compounds with the metabolic inhibitor, NIA16388 (propargyl propyl phenylphosphonate). For the nitromethylene analogues, including both benzyl and pyridylmethyl analogues, higher binding activity usually resulted in higher insecticidal activity. (C) 2000 Society of Chemical Industry.
A Convenient Procedure for the Reduction of Esters, Carboxylic Acids, Ketones and Aldehydes using Tetrabutylammonium Fluoride (or Triton B) and Polymethylhydrosiloxane
Drew, Mark D.,Lawrence, Nicholas J.,Fontaine, David,Sehkri, Lakhdar,Bowles, Stephen A.,Watson, William
, p. 989 - 991 (2007/10/03)
A range of carboxylic esters and acids have been converted efficiently to the corresponding alcohols with polymethylhydrosiloxane in the presence of catalytic tetrabutylammonium fluoride. The reduction of ketones and aldehydes with PMHS and other alkoxysilanes in the presence of TBAF or benzyltrimethylammonium hydroxide is also described.
5-amino or substituted amino 1,2,3-triazoles useful as antimetastatic agents
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, (2008/06/13)
This invention is directed to the method of treating patients with surgically excised tumors with a high probability of metastasis, such as melanoma and breast cancer, by administering to such patient a nontoxic therapeutically effective amount of a 5-amino or substituted amino, 1,2,3-triazoles which are disclosed as a new class of antimetastatic agents useful in such treatment.
5-Amino or substituted amino 1,2,3,-triazoles useful as antiproliferative agents
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, (2008/06/13)
5-Amino or substituted amino 1,2,3-triazoles are disclosed as a new class of antiproliferative agents useful in the treating and managing of psoriasis, inflammatory bowel syndrome, cutaneous leishmanilisis and certain types of cancer.
