- Conjugate addition of aryl nucleophiles to α,β-unsaturated cinnamic acid derivatives containing Evans type chiral auxiliaries
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Cinnamides containing oxazolidin-2-one type auxiliaries have been prepared. A novel pathway to chiral 4-aryl-6-methyl-3,4-dihydrocoumrines via the asymmetric conjugate addition of arylmagnesium bromides to these cinnamides is described.
- Leitis, Zigmārs,Lūsis, Viesturs
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p. 843 - 851
(2016/09/02)
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- Towards the total synthesis of marineosin A: Construction of the macrocyclic pyrrole and an advanced, functionalized spiroaminal model
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Herein, we describe the enantioselective construction of the 12-membered macrocyclic pyrrole core of marineosin A in 5.1 % overall yield from (S)-propylene oxide. The route features a key Stetter reaction to install a 1,4-diketone, which is subjected to Paal-Knorr pyrrole synthesis and ring-closing metathesis to afford the macrocycle. A divergence point in the synthetic scheme also enabled access to a highly functionalized spiroaminal model system through an acid-mediated hydroxy oxo amide cyclization strategy. Copyright
- Aldrich, Leslie N.,Berry, Cynthia B.,Bates, Brittney S.,Konkol, Leah C.,So, Miranda,Lindsley, Craig W.
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supporting information
p. 4215 - 4218
(2013/07/26)
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- Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis
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Herein, we report on the identification of nonbasic, potent, and highly selective, nitrile-containing cathepsin K (Cat K) inhibitors that are built on our previously identified cyclohexanecarboxamide core structure. Subsequent to our initial investigation
- Robichaud, J?el,Black, W. Cameron,Thérien, Michel,Paquet, Julie,Oballa, Renata M.,Bayly, Christopher I.,McKay, Daniel J.,Wang, Qingping,Isabel, Elise,Léger, Serge,Mellon, Christophe,Kimmel, Donald B.,Wesolowski, Gregg,Percival, M. David,Massé, Frédéric,Desmarais, Sylvie,Falgueyret, Jean-Pierre,Crane, Sheldon N.
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experimental part
p. 6410 - 6420
(2009/10/23)
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- A short approach to the bicyclo[4.3.0]nonane fragment of stawamycin
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The bicyclo[4.3.0]nonane (C11-C21) fragment of stawamycin has been prepared by a sequence involving 11 steps (10% overall yield) from methyl (R)-(-)-3-hydroxy-2-methylpropionate. Key steps are a Pd-catalysed Stille coupling reaction
- Dias, Luiz C.,Melgar, Gliseida Z.,Jardim, Luciana S. A.
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p. 4427 - 4431
(2007/10/03)
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- SELECTED CGRP ANTAGONISTS, METHOD FOR PRODUCTION AND USE THEREOF AS MEDICAMENT
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The invention relates to CGRP antagonists of general formula (I), in which A, U, V, W, X and R1 to R 3 are as defined in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures, salts, hydrates of the salts, in particular the physiologically-acceptable salts thereof with inorganic or organic acids, medicaments containing said compounds and the use and methods for production thereof.
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Page/Page column 122
(2008/06/13)
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