- CYCLIC SULFAMIDE COMPOUNDS AND METHODS OF USING SAME
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The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.
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Page/Page column 387
(2018/09/21)
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- Visible-Light-Mediated Rose Bengal-Catalyzed α-Hydroxymethylation of Ketones with Methanol
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A visible-light-mediated α-hydroxymethylation of ketones using methanol as the hydroxymethylating reagent has been developed. Using 1 mol% rose bengal as the photosensitizer and air as the green oxidant, the reactions proceeded smoothly at room temperature. Experimental studies indicate the reaction proceeded via a radical pathway. (Figure presented.).
- Yang, Jingya,Xie, Dongtai,Zhou, Hongyan,Chen, Shuwen,Duan, Jiaokui,Huo, Congde,Li, Zheng
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supporting information
p. 3471 - 3476
(2018/09/12)
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- A chemoselective α-aminoxylation of aryl ketones: a cross dehydrogenative coupling reaction catalysed by Bu4NI
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Tetrabutyl ammonium iodide (TBAI) catalyzed α-aminoxylation of ketones using aq. TBHP as an oxidant has been accomplished. We have shown that the CDC (cross dehydrogenative coupling) reactions of ketones with N-hydroxyimidates such as N-hydroxysuccinimide (NHSI), N-hydroxyphthalimide (NHPI), N-hydroxybenzotriazole (HOBt) and 1-hydroxy-7-azabenzotriazole (HOAt) lead to the corresponding oxygenated products in good to moderate yields. The application of this method has been demonstrated by transforming a few coupled products into synthetically useful intermediates and products.
- Siddaraju, Yogesh,Prabhu, Kandikere Ramaiah
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supporting information
p. 11651 - 11656
(2015/12/08)
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- Catalyst-controlled regiodivergent C-H borylation of multifunctionalized heteroarenes by using iridium complexes
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The regiodivergent C-H borylation of 2,5-disubstituted heteroarenes with bis(pinacolato)diboron was achieved by using iridium catalysts formed in situ from [Ir(OMe)(cod)]2/dtbpy (cod=1,5-cyclooctadiene, dtbpy: 4,4′-di-tert-butyl-2,2′-bipyridine) or [Ir(OMe)(cod)]2/2 AsPh3. When [Ir(OMe)(cod)]2/dtbpy was used as the catalyst, borylation at the 4-position proceeded selectively to afford 4-borylated products in high yields (dtbpy system A). The regioselectivity changed when the [Ir(OMe)(cod)]2/2 AsPh3 catalyst was used; 3-borylated products were obtained in high yields with high regioselectivity (AsPh3 system B). The regioselectivity of borylation was easily controlled by changing the ligands. This reaction was used in the syntheses of two different bioactive compound analogues by using the same starting material. Minor adjustments, major differences: The regiodivergent C-H borylation of 2,5-disubstituted heteroarenes with bis(pinacolato)diboron was achieved by using iridium catalysts formed in situ from [Ir(OMe)(cod)]2/dtbpy (cod=1,5-cyclooctadiene, dtbpy: 4,4'-di-tert-butyl-2,2'-bipyridine) or [Ir(OMe)(cod)]2/2 AsPh3 (see scheme).
- Sasaki, Ikuo,Taguchi, Jumpei,Hiraki, Shotaro,Ito, Hajime,Ishiyama, Tatsuo
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supporting information
p. 9236 - 9241
(2015/06/16)
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- Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect
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A few thienyl substituted pyrazole derivatives were synthesized to aid in the characterization of the cannabinoid receptor antagonist and also to serve as potentially useful antiobesity agent. Structural requirements for selective CB1 receptor antagonistic activity of 5-thienyl pyrazole derivatives included the structural similarity with potent, specific antagonist rimonabant 1. Compound 3 has been identified as a hair growth stimulator and an antiobesity agent in animal models.
- Srivastava, Brijesh Kumar,Soni, Rina,Patel, Jayendra Z.,Joharapurkar, Amit,Sadhwani, Nisha,Kshirsagar, Samadhan,Mishra, Bhupendra,Takale, Vijay,Gupta, Sunil,Pandya, Purvi,Kapadnis, Prashant,Solanki, Manish,Patel, Harilal,Mitra, Prasenjit,Jain, Mukul R.,Patel, Pankaj R.
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scheme or table
p. 2546 - 2550
(2010/01/16)
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- Ytterbium(III) trifluoromethanesulfonate catalysed Friedel-Crafts acylation of substituted thiophenes
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Ytterbium(III) trifluoromethanesulfonate [Yb(OTf)3] has been used to catalyse Friedel-Crafts acylation of substituted thiophenes in different solvents to produce several intermediates of pharmaceuticals and pesticides with good yields. The amount of catalysis was discussed and Yb(OTf)3 could be reused without loss of activity.
- Su, Weike,Jin, Can
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p. 694 - 695
(2007/10/03)
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