- Synthesis of some fused β-carbolines including the first example of the pyrrolo[3,2-c]-β-carboline system
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Condensation of 1-methyl-β-carboline-3-carbaldehyde with ethyl azidoacetate and subsequent thermolysis of the resulting azidopropenoate was used to [c] annulate a pyrrole ring onto the β-carboline moiety, thus producing the first example of the pyrrolo[3,
- Condie, Glenn C.,Bergman, Jan
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Read Online
- AZAINDOLE COMPOUNDS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS
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Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
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Page/Page column 82
(2008/06/13)
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- PHOSPHOLIPASE INHIBITORS, INCLUDING MULTI-VALENT PHOSPHOLIPASE INHIBITORS, AND USE THEREOF, INCLUDING AS LUMEN-LOCALIZED PHOSPHOLIPASE INHIBITORS
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The present invention provides methods and compositions for the treatment of phospholipase-related conditions. In particular, the invention provides a method of treating insulin-related, weight-related conditions and/or cholesterol-related conditions in an animal subject. The method generally involves the administration of a non-absorbed and/or effluxed phospholipase A2 inhibitor that is localized in a gastrointestinal lumen.
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Page/Page column 226
(2010/11/27)
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- Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors
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Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.
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Page/Page column 120-121
(2010/11/27)
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- Carbodiimide-mediated preparation of the tricyclic pyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine ring system and its application to the synthesis of the potent antitumoral marine alkaloid variolin B and analog
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A total synthesis of the marine alkaloid variolin B has been completed in 13 steps in an overall yield of 6.5% from 3-formyl-4-methoxypyridine. Our approach is based on the sequential formation of the 7-azaindole ring, the tricyclic pyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine ring system, and finally installation of the 2-aminopyrimidine ring at C5. The required 7-azaindole ring appropriately substituted is formed by a modified indole synthesis involving a nitrene insertion process (two steps). Formation of the annelated pyrimidine ring is achieved by two routes both involving a carbodiimide-mediated cyclization process, which allow incorporation of the amine functionality at C9 of the core tricyclic (six steps). Installation of the northeast 2-aminopyrimidine ring at C5 is performed using the Bredereck protocol (three steps). Ultimate, thermal decarboxylation with concomitant O-methyl deprotection and further N-benzyl deprotection by the action of triflic acid completed the synthesis of the target natural product variolin B.
- Molina, Pedro,Fresneda, Pilar M.,Delgado, Santiago
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p. 489 - 499
(2007/10/03)
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- Synthetic studies towards the 2-aminopyrimidine alkaloids variolins and meridianins from marine origin
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A nine-step synthesis of 9-amino-4-methoxypyrido[3',2':4,5]pyrrolo[1,2- c]pyrimidine, a tricyclic ring system present in the marine alkaloids variolins is described. The natural marine products meridianins C-E have been synthesized for the first time starting from N-protected 3-acylindoles. (C) 2000 Elsevier Science Ltd.
- Fresneda, Pilar M.,Molina, Pedro,Delgado, Santiago,Bleda, Juan A.
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p. 4777 - 4780
(2007/10/03)
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