42268-68-8Relevant academic research and scientific papers
Chemoproteomics-Enabled De Novo Discovery of Photoswitchable Carboxylesterase Inhibitors for Optically Controlled Drug Metabolism
Dwyer, Brendan G.,Wang, Chao,Abegg, Daniel,Racioppo, Brittney,Qiu, Nan,Zhao, Zhensheng,Pechalrieu, Dany,Shuster, Anton,Hoch, Dominic G.,Adibekian, Alexander
, p. 3071 - 3079 (2021)
Herein, we report arylazopyrazole ureas and sulfones as a novel class of photoswitchable serine hydrolase inhibitors and present a chemoproteomic platform for rapid discovery of optically controlled serine hydrolase targets in complex proteomes. Specifica
Substituted Propargylamines—Acid Corrosion Inhibitors for Steel in Petroleum Industry
Avdeev, Ya. G.,Dzhafarova, U. Sh.,Shatirova, M. I.
, p. 1088 - 1096 (2021/11/30)
Secondary and tertiary amines of the acetylene series of various structures (14 compounds) were synthesized based on propargylamine. The possibility of a significant inhibition with these substances of low-carbon steel corrosion in hot solutions of hydrochloric acid was established. The protective effect of acetylenic amines rose with an increase in their content in an aggressive environment and with an increase in its temperature. The maximum protection effect is provided by tertiary amines containing 2,3-epoxypropyl or 2,3-epithiopropyl as a substituent. The presence of chemically active epoxy and epithio groups in the structure of these acetylenic compounds promoted the stimulation of their polymerization on the steel surface through the opening of C≡C bonds, leading to the rapid formation of a protective polymer film on it.
West request acid bei geleg sandbank and intermediate preparation method
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Paragraph 0077-0081, (2019/02/26)
The invention relates to a preparation method of besigliptin and its intermediate, and concretely relates to a preparation method of an azadicyclic compound besigliptin and its key intermediate. The preparation method comprises the following steps: carrying out step a, step b and step c to prepare the key intermediate compound of formula VII, carryin gout isomer resolution and protective group removal on the compound of formula VII to obtain a compound of formula XV, coupling the compound of formula XV with the compound of formula XIII, and salifying to form a target compound I. The preparation method has the advantages of substantial reduction of the production cost, simple production flow, yield increase, and suitableness for industrial production.
A two-directional strategy for the diversity-oriented synthesis of macrocyclic scaffolds
O'Connell, Kieron M. G.,Beckmann, Henning S. G.,Laraia, Luca,Horsley, Helen T.,Bender, Andreas,Venkitaraman, Ashok R.,Spring, David R.
, p. 7545 - 7551 (2012/10/29)
Macrocyclic compounds represent a structural class with exceptional potential for biological activity; however, they have historically been underrepresented in screening collections and synthetic libraries. In this article we report the development of a highly step-efficient strategy for the diversity-oriented synthesis of complex macrocyclic architectures, using a modular approach based on the two-directional synthesis of bifunctional linear precursors and their subsequent combination in a two-directional macrocyclisation process. In this proof of principle study, the synthesis of 14 such compounds was achieved. Cheminformatic analysis of the compounds produced suggests that they reside in biologically relevant regions of chemical space and the compounds were screened for activity against two cancer cell lines.
A dicationic ruthenium alkylidene complex for continuous biphasic metathesis using monolith-supported ionic liquids
Autenrieth, Benjamin,Frey, Wolfgang,Buchmeiser, Michael R.
, p. 14069 - 14078 (2013/01/15)
A dicationic ruthenium-alkylidene complex [Ru(dmf)3(IMesH 2)(=CH-2-(2-PrO)-C6H4)][(BF4) 2] (1; IMesH2=1,3-dimesitylimidazolin-2-ylidene) has been prepared and used in continuous metathesis reactions by exploiting supported ionic-liquid phase (SILP) technology. For these purposes, ring-opening metathesis polymerization (ROMP)-derived monoliths were prepared from norborn-2-ene, tris(norborn-5-ene-2-ylmethyloxy)methylsilane, and [RuCl 2(PCy3)2(CHPh)] (Cy=cyclohexyl) in the presence of 2-propanol and toluene and surface grafted with norborn-5-en-2-ylmethyl-N,N, N-trimethylammonium tetrafluoroborate ([NBE-CH2-NMe 3][BF4]). Subsequent immobilization of the ionic liquid (IL), 1-butyl-2,3-dimethylimidazolium tetrafluoroborate ([BDMIM][BF 4]), containing ionic catalyst 1 created the SILP catalyst. The use of a second liquid transport phase, which contained the substrate and was immiscible with the IL, allowed continuous metathesis reactions to be realized. High turnover numbers (TONs) of up to 3700 obtained in organic solvents for the ring-closing metathesis (RCM) of, for example, N,N-diallyltrifluoroacetamide, diethyl diallylmalonate, diethyl di(methallyl)malonate, tert-butyl-N,N- diallylcarbamate, N,N-diallylacetamide, diphenyldiallylsilane, and 1,7-octadiene, as well as in the self-metathesis of methyl oleate, could be further increased by using biphasic conditions with [BDMIM][BF 4]/heptane. Under continuous SILP conditions, TONs up to 900 were observed. Due to the ionic character of the initiator, catalyst leaching into the transport phase was very low (4]/1, the recycled support material again qualified for utilization in continuous metathesis reactions. Copyright
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 30, (2012/08/08)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 33, (2012/07/28)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
BICYCLIC CYLOPENTANONE AND CYCLOPENTENONE DERIVATIVES AS POTENT ACTIVATORS OF HSF
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Page 30-31, (2010/11/30)
A compound of formula (I), (II), (III) or (IV); wherein R1 and R2 are each, independently, hydrogen or an alkyl group containing 1-4 carbon atoms; R3 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group co
Organolanthanide-catalyzed intra- and intermolecular tandem C-N and C-C bond-forming processes of aminodialkenes, aminodialkynes, aminoalkeneynes, and aminoalkynes. New regiospecific approaches to pyrrolizidine, indolizidine, pyrrole, and pyrazine skeleto
Li, Yanwu,Marks, Tobin J.
, p. 1757 - 1771 (2007/10/03)
This contribution describes catalytic tandem C-N and C-C bond-forming reactions involving the intramolecular hydroamination/bicyclization and intermolecular hydroamination/cyclization of olefins and alkynes using the organolanthanide complexes Cp'2/
The Synthesis of Nitrogen Heterocycles via the Intramolecular Khand Reaction: Formation of Tetra- and Hexa-hydrocyclopentapyrrol-5(1H)-ones and Hexahydro-6H-2-pyrindin-6-ones
Brown, Scott W.,Pauson, Peter L.
, p. 1205 - 1209 (2007/10/02)
Azabicyclooctenones and azabicyclononenones have been obtained by cyclisation of hexacarbonyldicobalt complexes of aza-heptenynes and -octenynes respectively.An unusual feature of the cyclisation of N-acyl-4-azahept-1-en-6-ynes is the extens
