- Cobalt-Catalyzed Desymmetric Isomerization of Exocyclic Olefins
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Chiral cyclic olefins, 1-methylcyclohexenes, are versatile building blocks for the synthesis of pharmaceuticals and natural products. Despite the prevalence of these structural motifs, the development of efficient synthetic methods remains an unmet challenge. Herein we report a novel desymmetric isomerization of exocyclic olefins using a series of newly designed chiral cobalt catalysts, which enables a straightforward construction of chiral 1-methylcyclohexenes with diversified functionalities. The synthetic utility of this methodology is highlighted by a concise and enantioselective synthesis of a natural product, β-bisabolene. The versatility of the reaction products is further demonstrated by multifarious derivatizations.
- Lan, Yu,Liu, Qiang,Liu, Shihan,Liu, Xufang,Rong, Xianle
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supporting information
p. 20633 - 20639
(2021/12/17)
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- IMIDAZOPYRROLOPYRIDINE AS INHIBITORS OF THE JAK FAMILY OF KINASES
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2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
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Page/Page column 223; 259; 260
(2018/07/05)
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- S1P MODULATING AGENTS
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Compounds of formula (I) can modulate the activity of one or more S 1P receptors. Sphingosine 1-phosphate (S IP) is a lysophospholipid mediator that evokes a variety of cellular responses by stimulation of five members of the endothelial cell differentiation gene (EDG) receptor family, namely S1P1, S1P2, S1P3, S1P4, and S1P5 (formerly EDG1, EDG5, EDG3, EDG6 and EDG8). The EDG receptors are G-protein coupled receptors (GPCRs) and on stimulation propagate second messenger signals via activation of heterotrimeric G-protein alpha (Ga.) subunits and beta-gamma (G()y) dimers.
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Page/Page column 57-58
(2014/08/19)
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- COMPOUNDS THAT ARE S1P MODULATING AGENTS AND/OR ATX MODULATING AGENTS
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Compounds of formula (I) can modulate the activity of one or more S1P receptors and/or the activity of autotaxin (ATX).
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Page/Page column 143
(2014/02/16)
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- S1P MODULATING AGENTS
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Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
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Page/Page column 133
(2012/08/28)
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- Diastereoselectivity control of the radical carboazidation of substituted methylenecyclohexanes
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A systematic study of the diastereoselectivity of the radical carboazidation of methylenecyclohexane derivatives is presented. Several substitution patterns leading to a high level of stereocontrol have been identified. Axial attack is the preferred reaction pathway for cyclohexyl radicals, and excellent stereoselectivities can be obtained by introducing an axial substitutent at position 2. In this case, a second equatorial substituent at position 2 may be tolerated without a large detrimental effect on the diastereoselectivity. Finally, a high level of equatorial attack is observed with a very bulky substituent at position 2.
- Cren, Sylvaine,Schar, Pascal,Renaud, Philippe,Schenk, Kurt
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supporting information; experimental part
p. 2942 - 2946
(2009/09/06)
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- COMPOUNDS FOR INHIBITING KSP KINESIN ACTIVITY
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The present invention provides compounds of Formula (I) (wherein R1, R3, X, W, Z and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
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Page/Page column 167; 168
(2010/11/23)
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- Silicon and tin-directed Tiffeneau-Demjanov reaction
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Silicon and tin substituents surprisingly have only a moderate directing effect on the Tiffeneau-Demjanov reaction. The low selectivity is rationalised as being due to the reactive nature of the diazonium ion leaving group, the weaker oxydiazene leaving g
- Chow, Leonie,McClure, Melanie,White, Jonathan
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p. 648 - 650
(2007/10/03)
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