106511-71-1Relevant academic research and scientific papers
Pentamethylphenyl (Ph*) and Related Derivatives as Useful Acyl Protecting Groups for Organic Synthesis: A Preliminary Study
Cheong, Choon Boon,Frost, James R.,Donohoe, Timothy J.
, p. 1828 - 1832 (2020/10/06)
A study of acyl protecting groups derived from the Ph? motif is reported. While initial studies indicated that a variety of functional groups were not compatible with the Br 2-mediated cleavage conditions required to release the Ph? group, strategies involving the use of different reagents or a modification of Ph? itself (Ph*OH) were investigated to solve this problem.
α,α-Alkylation-Halogenation and Dihalogenation of Sulfoxonium Ylides. A Direct Preparation of Geminal Difunctionalized Ketones
Gallo, Rafael D. C.,Ahmad, Anees,Metzker, Gustavo,Burtoloso, Antonio C. B.
supporting information, p. 16980 - 16984 (2017/11/27)
A one-pot alkylation–halogenation of ketosulfoxonium ylides in the presence of alkyl halides is described. The method furnishes several gem-difunctionalized haloketones (an alkyl and F, Cl, Br, or I) in good yields. Replacing alkyl halides with a mixture of electrophilic halogen species and various halide anions led to gem-dihalogenated ketones containing a combination of the same or two different halogens. Kinetic isotopic effects as well as reaction kinetic experiments give insight to the mechanism of these reactions.
2, 4, 5-trisubstituted selenazole class compound and its preparation method, composition and use thereof
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, (2016/11/17)
The invention relates to 2,4,5-trisubstituted selenazole compounds and a preparation method, a composition and application thereof, in particular to compounds in a formula (I), or all possible isomers, predrugs, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein each substituent is shown as the description. The invention also relates to a method for preparing the compounds in the formula (I), medicinal compositions comprising the compounds in the formula (I), and application of the compounds in the formula (I) or the medicinal compositions in preparation of medicines for treating and/or preventing phospholipid transfer protein (PLTP) activity increase and/or diseases or syndromes related with the phospholipid transfer protein activity increase. The compounds in the formula (I) have good effect of inhibiting the PLTP activity and/or cholesteryl ester transfer protein (CETP) activity of blood plasma, and can be used for treating diseases on the basis.
2,4,5-Trisubstituted thiazole derivatives: A novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase
Xu, Zhongliang,Ba, Mingyu,Zhou, Hua,Cao, Yingli,Tang, Chaojun,Yang, Ying,He, Ricai,Liang, Yu,Zhang, Xuemei,Li, Zhenzhong,Zhu, Lihong,Guo, Ying,Guo, Changbin
, p. 27 - 42 (2014/08/18)
Novel 2,4,5-trisubstituted thiazole derivatives (TSTs) were designed and synthesized as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Among the thirty-eight synthesized target compounds, thirty TSTs showed potent inhibition against HIV-1 replication in wild type HIV-1 at submicromolar concentrations (from 0.046 to 9.59 μM). Compounds 21, 23 and 24 were also tested on seven NNRTI-resistant HIV-1 strains, and all exhibited inhibitory effects with fold changes in IC50 ranging from 2.6 to 111, which were better than those of nevirapine (15.6-fold-371-fold). Docking simulations of compound 24 revealed a reasonable mechanism for the binding mode, and three-dimensional quantitative structure activity relationship (3-DQSAR) studies on this novel series of TST further elucidated the structure-activity relationship (SAR). The results suggested the great potential of TSTs as a novel class of NNRTIs with antiviral efficacy and a good resistance profile.
Kinetic diastereomer differentiation in Au(III)- and Bi(III)-catalyzed benzylic arylation: Concise and stereocontrolled synthesis of 2-amino-1,1-diarylalkanes
Chenard, Etienne,Hanessian, Stephen
supporting information, p. 2668 - 2671 (2014/06/09)
Benzylic alcohols carrying an adjacent α-nitro or α-azido group on the alkane chain are converted into syn-1,1-diaryl-2-nitro- and 2-azidoalkanes with electron-rich arenes in stereoselective reactions catalyzed by Bronsted and Lewis acids. Gold(III) chloride and bismuth(III) triflate were found to be especially efficient as catalysts, showing kinetically controlled differentiation in the reactivity of diastereomeric α-substituted benzyl alcohols. Applications to therapeutically relevant syn- and anti- 2-amino-1,1-diarylalkanes are projected.
Synthesis of a series of novel 2,4,5-trisubstituted selenazole compounds as potential PLTP inhibitors
Ling, Cui,Zheng, Zhibing,Jiang, Xian Cheng,Zhong, Wu,Li, Song
scheme or table, p. 5123 - 5125 (2010/10/19)
Based on a homology-modeled structure of PLTP and characteristic structural features of reported cholesteryl ester transfer protein (CETP) inhibitors, we designed and synthesized a novel series of 2,4,5-trisubstituted selenazole compounds. Biological evaluation reveals that compounds 12 and 17 exhibit favorable PLTP activity, and their IC50s are 8 μM and 10 μM, respectively.
2,4,5-TRISUBSTITUTED THIAZOLE COMPOUNDS,PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES THEREOF
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Page/Page column 19-20, (2009/04/23)
The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.
TRISUBSTITUTED THIAZOLE COMPOUNDS, PREPARATIONS METHODS, PHARMACEUTICAL COMPOSITIONS AND MEDICALS USES THEREOF
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Page/Page column 14, (2009/12/23)
The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.
3-ARYL-2-BENZYL-1,2-DIHYDROQUINOXALINES
Orlov, V. D.,Insuasti, B.,Kolos, N. N.
, p. 685 - 687 (2007/10/02)
The reaction of 1,2-phenylenediamine with 2-bromo-1,3-diaryl-1-propanones led to stable and crystalline 3-(4-R-phenyl)-2-(4-R'-benzyl)-1,2-dihydroquinoxalines.
Some New Thiazole Derivatives from Dihydrochalcones
Ahluwalia, V. K.,Kaila, Neelu,Bala, Shashi
, p. 502 - 504 (2007/10/02)
α-Bromo-α,β-dihydrochalcones on condensation with thiourea and ammonium dithiocarbamate afford 2-amino- and 2-mercapto-4-aryl-5-arylmethylthiazoles, respectively.The starting α-bromo derivatives are obtained by bromination of corresponding dihydrochalcone
