A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists
Moderately potent, selective S1P1 receptor agonists identified from high-throughput screening have been adapted into lipophilic tails for a class of orally bioavailable amino acid-based S1P1 agonists represented by 7. Many of the new
Hale, Jeffrey J.,Lynch, Christopher L.,Neway, William,Mills, Sander G.,Hajdu, Richard,Keohane, Carol Ann,Rosenbach, Mark J.,Milligan, James A.,Shei, Gan-Ju,Parent, Stephen A.,Chrebet, Gary,Bergstrom, James,Card, Deborah,Ferrer, Marc,Hodder, Peter,Strulovici, Berta,Rosen, Hugh,Mandala, Suzanne
The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
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Page/Page column 18-19
(2010/11/25)
Preparation of pyrrole-2-carboxylates with electron-withdrawing groups at the 4-position
Reaction of α-trifluoromethyl, α-cyano, and α-ethoxycarbonyl alkenyl sulfones with ethyl isocyanoacetate in the presence of a base gave 4- substituted pyrrole-2-carboxylates in moderate to good yields.
Reactivity of β-(trifluoromethyl) acroleins towards primary alkyl (or aryl) amines: synthesis of trifluoromethyl)-1-aza-1,3-dienes and secondary (trifluoromethyl) allylamines
Vilsmeier's reaction on trifluoroketones leads to β-chloro-β(trifluoromethyl)acroleins.The addition of primary alkyl- or aryl-amines to these acroleins leads in all cases to the formation of stable (trifluoromethyl)-1-aza-1,3-dienes which can be transform
Selmi, A.,Gaied, M. M. El,Alvernhe, G.
p. 1 - 8
(2007/10/02)
Synthesis of γγγ-trifluorocarbonyl compounds
γγγ-Trifluorocarbonyl compounds are easily obtained in a good yield by introduction of the 1,1,1-trifluoroethyl moiety (CF3-CH2-) on the α-methylene group of a ketone.
Laurent,Lesniak
p. 8091 - 8092
(2007/10/02)
A new and efficient synthesis of trifluoroalkyl aldehydes or ketones from the same starting material
4,4,4-trifluoroacroleines 2 have been converted specifically by tributyl tin hydride to aldehyders 3 or ketones 4, according to the catalyst and conditions employed.
Laurent, Andre J.,Leniak, Stanislaw
p. 3311 - 3314
(2007/10/02)
Zur Synthese eines trifluormethylsubstituierten β-Thioxoaldehyds und seiner Derivate
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Weissenfels, Manfred,Pulst, Manfred,Greif, Dieter,Hoffmann, Rene,Laurent, Andre,Mison, Pierre
p. 247 - 248
(2007/10/02)
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