- ANTI-ENTEROVIRUS 71 THIADIAZOLIDINE DERIVATIVE
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Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof; and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
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Paragraph 0583
(2017/03/28)
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- Double axial chirality promoted asymmetric [2,3] Stevens rearrangement of N-cinnamyl l-alanine amide-derived ammonium ylides
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The base-induced asymmetric [2,3] Stevens rearrangement of N-cinnamyl tetraalkylammonium ylides derived from l-alanine amides proceeds via a double axially chiral intermediate to afford the corresponding α-substituted alanine derivatives with high enantio- and diastereoselectivities. the Partner Organisations 2014.
- Tayama, Eiji,Naganuma, Noriko,Iwamoto, Hajime,Hasegawa, Eietsu
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supporting information
p. 6860 - 6862
(2014/06/23)
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- 4'-AMINO CYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): formula (I) wherein Cy is selected from formula (Il) and wherein R1, R2, R3, Q, G, Ar, m, n and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 127; 128
(2010/04/06)
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- Ruthenium-lewis acid catalyzed asymmetric diels-alder reactions between dienes and α,β-unsaturated ketones
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The complex [Ru(Cp)(R,R-BIPHOP-F)(acetone)][SbF6],(R,R)-1a. was used as catalyst for asymmetric Diels-Alder reactions between dienes (cyclopentadiene, methylcyclopentadienc, isoprene, 2,3-dimethylbutadiene) and α,β-unsaturated ketones (methyl vinyl ketone (MVK). ethyl vinyl ketone, divinyl ketone, α-bromovinyl methyl ketone and α-chlorovinyl methyl ketone). The cycloaddition products were obtained in yields of 50-_90% and with enantioselectivities up to 96% ee. Ethyl vinyl ketone, divinyl ketone and the halogenated vinyl ketones worked best and their reactions with acyclic dienes consistently provided products with >90% ee. α-Chlorovinyl methyl ketone performed better than α-bromovinyl methyl ketone. The reaction also provided a [4.3.1]bicyclic ring system in 95% ee through an intramolecular cycloaddition reaction. Crystal structure determinations of [Ru(Cp)((S,S)-BIPHOP-F)(mvk)]-[SbF6], (S,S)-1b, and [Ru(Cp)((R,R)-Me4BIPHOP-F)(acrolein)][SbF6], (R,R)-2b, provided the basis for a rationalization of the asymmetric induction.
- Rickerby, Jenny,Vallet, Martial,Bernardinelli, Gerald,Viton, Florian,Kuendig, E. Peter
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p. 3354 - 3368
(2008/03/27)
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- Asymmetric construction of a quaternary carbon center by tandem [4 + 2]/[3 + 2] cycloaddition of a nitroalkene. The total synthesis of (-)-mesembrine
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An efficient, total synthesis of the Sceletium alkaloid (-)-mesembrine is accomplished in seven steps and 19% yield from a functionalized nitroalkene (itself prepared in six steps and 34% yield from ethyl 3-bromopropionate). The construction of the octahydroindole framework of mesembrine features a tandem inter [4 + 2]/intra [3 + 2] cycloaddition of a 2,2-disubstituted 1-nitroalkene and a chiral vinyl ether derived from (1R,2S)-2-(1-methyl-1-phenylethyl)cyclohexanol as the central strategic element. The two stereogenic centers of the natural product, which include a benzylic, quaternary center, were established in 26/1 selectivity in the tandem process.
- Denmark, Scott E.,Marcin, Lawrence R.
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p. 1675 - 1686
(2007/10/03)
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- A SIMPLE METHOD FOR THE PRODUCTION OF 1,5-DIHALOGENO-3-PENTANONES AND 1-BROMO-3-PENTANONE - PRECURSORS OF DIVINYL AND ETHYL VINYL KETONES
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The reaction of methyl 3-halogenopropionates with ethylmagnesium bromide in the presence of catalytic amounts of tetraisopropoxytitanium gave the corresponding 1-(2-halogenoethyl)cyclopropanols, the bromination of which with N-bromosuccinimide led to high yields of 1,5-dihalogeno-3-pentanones. 1-Bromo-3-pentanone was obtained by the acid-catalyzed opening of the three-membered ring of 1-(2-bromoethyl)cyclopropanol and also by the bromination of 1-ethylcyclopropanol.The reactions of 1,5-dibromo-3-pentanone with sodium carbonate and sodium sulfide led to good yields of divinyl ketone and 4-tetrahydrothiopyrone respectively.
- Sviridov, S. V.,Vasilevskii, D. A.,Kulinkovich, O. G.
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p. 1251 - 1253
(2007/10/02)
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