- CYCLIC VINYLOGOUS AMIDES AS BROMODOMAIN INHIBITORS
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Cyclic vinylogous amides of Formula (I) are disclosed. The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are in
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Paragraph 0065
(2015/03/16)
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- Direct amino acid-catalyzed cascade biomimetic reductive alkylations: Application to the asymmetric synthesis of Hajos-Parrish ketone analogues
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A direct amino acid-catalyzed chemo- and enantioselective process for the double cascade synthesis of highly substituted 2-alkyl-cyclopentane-1,3-diones, 2-alkyl-3-methoxy-cyclopent-2-enones and Hajos-Parrish (H-P) ketone analogs is presented via reductive alkylation chemistry. For the first time, we have developed a single-step alkylation of cyclopentane-1,3-dione with aldehydes/ketones and a Hantzsch ester through an organocatalytic reductive alkylation strategy. A direct combination of amino acid-catalyzed cascade olefination-hydrogenation and cascade Robinson annulations of cyclopentane-1,3-dione, aldehydes/ketones, a Hantzsch ester and methyl vinyl ketone furnished the highly functionalized H-P ketone analogues in good to high yields and with excellent enantioselectivities. Many of the reductive alkylation products have shown direct applications in pharmaceutical chemistry.
- Ramachary, Dhevalapally B.,Kishor, Mamillapalli
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supporting information; experimental part
p. 4176 - 4187
(2009/02/07)
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