- Catalyst-free and metal-free electrophilic bromoamidation of unactivated olefins using the N-bromosuccinimide/sulfonamide Protocol
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An efficient, catalyst-free, and metal-free bromoamidation of unactivated olefins has been developed. 4-(Trifluoromethyl)benzenesulfonamide and N-bromosuccinimide were used as the nitrogen and halogen sources, respectively. The methodology is applicable to both cyclic and aliphatic olefins.
- Yu, Wesley Zongrong,Chen, Feng,Cheng, Yi An,Yeung, Ying-Yeung
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p. 2815 - 2821
(2015/03/18)
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- Facile, efficient, and catalyst-free electrophilic aminoalkoxylation of olefins: Scope and application
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A new one-pot electrophilic aminoalkoxylation reaction using olefin, cyclic ether, amine, and N-bromosuccinimide has been developed. The olefinic substrates and the cyclic ether partners can be flexibly varied to produce a range of amino ether derivatives. This novel protocol has been applied in the facile and efficient synthesis of biologically active morpholine compounds.
- Zhou, Ling,Tan, Chong Kiat,Zhou, Jing,Yeung, Ying-Yeung
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supporting information; experimental part
p. 10245 - 10247
(2010/09/07)
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- Substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes as β3-adrenergic receptor agonists: Design, synthesis, biological evaluation and pharmacophore modeling
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In search of potent β3-adrenergic receptor agonists, a series of novel substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes has been synthesized and evaluated for their β3-adrenergic receptor agonistic activity (ranging from -17.73% to 90.64% inhibition at 10 μM) using well established Human SK-N-MC neuroblastoma cells model. Four molecules viz. 11, 15, 22 and 23 showed β3-AR agonistic IC50 value of 0.55, 0.59, 1.18 and 1.76 μM, respectively. These four candidates have been identified as possible leads for further development of β3-adrenergic receptor agonists for obesity and Type-II diabetes pharmacotherapy. The free OH and NH functions are found to be essential for β3-adrenergic receptor agonistic activity. Among the synthesized β3-adrenergic receptor agonists having 1,2,3,4-tetrahydroquinoline scaffold, the N-benzyl group is found to be superior over N-arylsulfonyl group. A putative pharmacophore model has been modeled considering the above four active molecules which distinguishes well between the active and inactive molecules.
- Shakya, Neeraj,Roy, Kuldeep K.,Saxena, Anil K.
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experimental part
p. 830 - 847
(2009/07/25)
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- Steroidal anaesthetics of the pregnane and 19-norpregnane series
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Steroid anaesthetics of the pregnane and 19-norpregnane series are described, the steroids having a 3α-hydroxy group, a 17α-hydrogen atom, a 20-oxo group and at the 21-position a cyano, azido or basic amino group.
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