- Iodine-catalyzed oxidative multiple C-H bond functionalization of isoquinolines with methylarenes: An efficient synthesis of isoquinoline-1,3,4(2: H)-triones
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An iodine-catalyzed multiple C-H bond functionalization of isoquinolines with methylarenes via a successive benzylic sp3 C-H iodination/N-benzylation/amidation/double sp2 C-H oxidation sequence is developed. This reaction utilizes un
- Zhu, Di,Luo, Wen-Kun,Yang, Luo,Ma, Da-You
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- Mechanistic Investigation of Castagnoli-Cushman Multicomponent Reactions Leading to a Three-Component Synthesis of Dihydroisoquinolones
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The mechanisms for the three- and four-component variants of the Castagnoli-Cushman reaction (CCR) have been investigated. A series of crossover experiments were conducted to probe the structure and reactivity of known amide-acid intermediates for the thr
- Howard, Sara Y.,Di Maso, Michael J.,Shimabukuro, Kristin,Burlow, Noah P.,Tan, Darlene Q.,Fettinger, James C.,Malig, Thomas C.,Hein, Jason E.,Shaw, Jared T.
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p. 11599 - 11607
(2021/09/02)
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- Enantioselective synthesis of isoquinoline-1,3(2: H,4 H)-dione derivatives via a chiral phosphoric acid catalyzed aza-Friedel-Crafts reaction
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A highly enantioselective aza-Friedel-Crafts reaction of structurally new ketimines with indoles and pyrrole is developed by using a chiral phosphoric acid as the catalyst. This protocol enables the first enantioselective synthesis of isoquinoline-1,3(2H,
- You, Yong,Lu, Wen-Ya,Xie, Ke-Xin,Zhao, Jian-Qiang,Wang, Zhen-Hua,Yuan, Wei-Cheng
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supporting information
p. 8478 - 8481
(2019/07/22)
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- INHIBITORS OF IRES-MEDIATED PROTEIN SYNTHESIS
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This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
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Page/Page column 38; 43
(2017/12/18)
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- Flower-shaped ZnO nanoparticles as an efficient, heterogeneous and reusable catalyst in the synthesis of N-arylhomophthalimides and benzannelated isoquinolinones
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A simple and green protocol, developed utilizing an efficient, heterogeneous and recyclable catalyst, i.e. zinc oxide nanoparticles (ZnO NPs)-mediated synthesis of N-arylhomophthalimides and benzannelated isoquinolinones, is reported. The structures of th
- Krishnakumar, Varadhan,Kumar, Kesarla Mohan,Mandal, Badal Kumar,Khan, Fazlur-Rahman Nawaz
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p. 1881 - 1892
(2013/02/22)
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- On the reactions of 1,3-isoquinolinediones with singlet oxygen
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Reactions of 1,3-isoquinolinediones 5 and 4-alkylated 1,3- isoquinolinediones 13 with singlet oxygen are entirely dominated by their enolization and proceed smoothly in benzene in the presence of pyridine as a base and a hydrogen bond acceptor. The products are triketones 6 and benzoisofuranones 7 for 5, and hydroperoxides 14, hydroxides 15 and benzoisofuranones 16 for 13. It was found that hydrolysis of 6 afforded the isoindolones 8 and not products 7, whereas alkaline cleavage of the hydroperoxide 14a yielded not only 16a, but also the isoindolone 19a, In view of these observations, an unusual [4+2] cycloaddition of the electron-rich enol 21 with singlet oxygen is proposed to be responsible for the formation of products 7 and 16, while products 6, 14 and 15 arise from both the [4+2] cycloaddition and the usual Schenck ene reaction pathways. This special diene reactivity of the isoquinolinone system towards singlet oxygen is further interpreted by frontier molecular orbital (FMO) interaction considerations.
- Ling, Ke-Qing,Ye, Jia-Hai,Chen, Xian-Yang,Ma, De-Jian,Xu, Jian-Hua
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p. 9185 - 9204
(2007/10/03)
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- Direct synthesis of imides from dicarboxylic acids using microwaves
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1,4- and 1,5-dicarboxylic acids, when treated with amines in a domestic microwave oven, afford good yields of the corresponding imides.
- Seijas, Julio A.,Vazquez-Tato, M. Pilar,Martinez, M. Montserrat,Nunez-Corredoira, Gonzalo
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p. 420 - 421
(2007/10/03)
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- Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: Novel inhibitors of COX-2
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A series of 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones was prepared. Members of this series are potent and selective inhibitors of cyclooxygenase- 2 (COX-2) in both microsomal and cellular assays. Two representatives demonstrated activity in the carrageenan-induced paw edema model in rats upon oral administration.
- Lazer, Edward S.,Sorcek, Ronald,Cywin, Charles L.,Thome, Diane,Possanza, Genus J.,Graham, Anne G.,Churchill, Laurie
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p. 1181 - 1186
(2007/10/03)
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- Synthetic approaches to 2-substituted 1-oxo- and 3-oxotetrahydroisoquinolines
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2-Substituted homophthalimides 2a-c were reduced regioselectively with sodium borohydride to carbinol-lactam intermediates 3a-c, which were dehydrated, followed by hydrogenation, to give 1-oxotetrahydroisoquinolines or 3,4-dihydroisoquinolin-1(2H)ones 5a-c. The isomeric 3-oxo-tetrahydroisoquinolines or 1,4-dihydroisoquinolin-3(2H)-ones 8a-i were obtained in satisfactory yields via heating 3-isochromanone (6) with the corresponding amines 7a-i in the presence of aluminum chloride.
- Cheng,Tsai,Lin
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