http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Achary, R.,Mathi, G.,Kim, S.,Hwang, J.,Kim, P. Royal Society Chemistry 2018 Organic & Biomolecular Chemistry Vol.16 No.9
<P>Treatment of the trifluoroacetyl enamides of dihydroisoquinolines 2 with diverse Grignard reagents afforded tertiary trifluoromethyl-carbinols 4 by facilitating the addition of tertiary carbinols to the beta-carbon of enamides 2. Based on the confirmed formation of vinylogous amides 3, the transformation likely proceeds via unique acyl group rearrangement to the beta-carbon of the enamide and subsequent nucleophilic addition of the Grignard reagent. Given the synthetic utility and novelty of this reaction, this work may open new avenues for the synthesis of pharmaceutically important tertiary trifluoromethylcarbinols on cyclic enamide systems.</P>
Discovery of novel tetrahydroisoquinoline-containing pyrimidines as ALK inhibitors
Achary, Raghavendra,Yun, Jeong In,Park, Chi Min,Mathi, Gangadhar Rao,Lee, Joo Yun,Ha, Jae Du,Chae, Chong Hak,Ahn, Sunjoo,Park, Chi Hoon,Lee, Chong Ock,Hwang, Jong Yeon,Yun, Chang-Soo,Jung, Hee Jung,Ch Pergamon 2016 Bioorganic & medicinal chemistry Vol.24 No.2
<P>Exploration of the two-position side chain of pyrimidine in LDK378 with tetrahydroisoquinolines (THIQs) led to discovery of 8 and 17 as highly potent ALK inhibitors. THIQs 8 and 17 showed encouraging in vitro and in vivo xenograft efficacies, comparable with those of LDK378. Although THIQ analogs (8a-o and 17a-i) prepared were not as active as their parent compounds, both 8 and 17 have significant inhibitory activities against various ALK mutant enzymes including G1202R, indicating that this series of compounds could be further optimized as useful ALK inhibitors overcoming the resistance issues found from crizotinib and LDK378. (C) 2015 Elsevier Ltd. All rights reserved.</P>
Achary, Raghavendra,Mathi, Gangadhar Rao,Lee, Dong Ho,Yun, Chang Soo,Lee, Chong Ock,Kim, Hyoung Rae,Park, Chi Hoon,Kim, Pilho,Hwang, Jong Yeon Elsevier 2017 Bioorganic & medicinal chemistry letters Vol.27 No.10
<P><B>Abstract</B></P> <P>In this study, a series of novel 2,4-diaminopyrimidines bearing fused tricyclic ring moiety was described for ALK inhibitor. The pyrazole, imidazole, 1,2,4-triazole, piperazine and phenanthridine moieties were employed at the 2-position of pyrimidine. Among the compounds synthesized, <B>28</B>, <B>29</B>, <B>36</B>, and <B>42</B> showed promising anti-ALK activities in enzymatic- and cell-based assays. <I>In vivo</I> H3122 xenograft model study showed that compound <B>29</B> effectively suppressed ALK-driven tumor growth, similar to the extent of ceritinib, suggesting that it could be used for a novel ALK inhibitor development.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Achary, Raghavendra,Jung, In-A,Lee, Hyeon-Kyu American Chemical Society 2018 Journal of organic chemistry Vol.83 No.7
<P>A tandem process, involving Rh(III)-catalyzed oxidative C-H olefination of enantiomerically enriched 4-aryl-benzo-1,3-sulfamidates and subsequent intramolecular aza-Michael cyclization has been developed. The reaction produces <I>trans</I>-benzosulfamidate-fused-1,3-disubstituted isoindolines as major products, in which the configurational integrity of the stereogenic center in the starting material is preserved. Further transformations of the benzosulfamidate-fused-1,3-disubstituted isoindolines are described.</P> [FIG OMISSION]</BR>
Achary, Raghavendra,Jung, In-A,Son, Se-Mi,Lee, Hyeon-Kyu American Chemical Society 2017 Journal of organic chemistry Vol.82 No.14
<P>A new method for the direct, stereoselective synthesis of highly functionalized 1,3-disubstituted isoindolines 6 from enantiomerically enriched cyclic 4-aryl-sulfamidate-5-carboxylates (5) is described. The process involves sulfamidate directed, Rh(III)-catalyzed tandem ortho CH olefination of the 4-aryl-sulfamidate-5-carboxylates and subsequent cyclization by aza-Michael addition. In the reaction, which generates trans-1,3-disubstituted isoindolines exclusively, the configurational integrity of the stereogenic center in the starting cyclic sulfamidate is completely retained in the product. Examples are provided which show that the cyclic sulfamidate moiety not only serves as a chiral directing group but also as a versatile handle for further functionalization of the generated isoindoline ring system.</P>
Divya Achari,Padmeshwary Rachipudi,Satishkumar Naik,Ramesh Karuppannan,Mahadevappa Kariduraganvar 한국공업화학회 2019 Journal of Industrial and Engineering Chemistry Vol.78 No.-
Chitosan-based polyelectrolyte complex membranes (PECMs) were developed by incorporatingpolystyrene sulfonic acid-co-maleic acid (PSSAMA) in the chitosan membrane matrix as a pervaporationmembrane by employing a solution technique. Fourier transform infrared (FTIR) spectroscopy, wideangleX-ray diffraction (WAXD), thermogravimetry analysis (TGA), differential scanning calorimetry(DSC), and scanning electron microscopy (SEM) were used to characterize the membranes. PECMs weretested for their potentiality to separate various azeotropic mixtures; water/ter-butanol, water/isopropanol, water/n-propanol and water/1, 4 dioxane at their azeotropic point. The PECMs containing9 mass% of PSSAMA manifest highest separation selectivity of 5352 with aflux of 4.145 10 2 kg /m2 h forthe azeotropic mixture of water/ter-butanol at 30 C. To confirm their stability at the higher temperature,the PECMs were assessed for pervaporation (PV) separation at 40, 50 and 60 C. For all PECMs totalfluxandflux of water appeared to be coinciding each other, signifying that PECMs could be used successfullyto break the azeotropic point of various azeotropic mixtures. The Arrhenius activation parameters weredetermined by diffusion and permeation values. The activation energy values procured for waterpermeation (Epw) were considerably lower than ter-butanol permeation (EpTBOH). The heat of sorption(DHs) values obtained for PECMs were negative, showing that Langmuir’s mode of sorption is dominant.