- TROPOLONE DERIVATIVES AND TAUTOMERS THEREOF FOR IRON REGULATION IN ANIMALS
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Disclosed are a series of compounds or their tautomers having a general structure represented by Formula (la), (lb), (Ila), (lIb), or (lIc) and pharmaceutically acceptable salts thereof. The present disclosure also relates to pharmaceutical compositions comprising said compounds or tautomers. The present disclosure further relates to a method of treating a disease or condition associated with iron dysregulation or dysfunctional iron homeostasis comprising administering to a subject in need thereof a therapeutically effective amount of Formula (la), (lb), (Ila), (lIb), or (lIc) compounds or tautomers.
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Page/Page column 197; 198
(2021/04/23)
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- HINOKITIOL ANALOGUES, METHODS OF PREPARING AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Disclosed are analogues of hinokitiol, methods for preparing them, and pharmaceutical compositions thereof. Also disclosed are methods for their use in treating iron-related diseases.
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- Efforts directed toward the synthesis of colchicine: Application of palladium-catalyzed siloxane cross-coupling methodology
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Colchicine is an important and synthetically challenging natural product. The key synthetic step in this approach to the synthesis of colchicine involved a palladium-catalyzed cross-coupling reaction between 5-bromotropolone (4) and an aryl siloxane to form the aryl-tropolone bond. The coupling of a variety of highly functionalized aryl siloxane derivatives was investigated and optimized coupling conditions were developed. It was discovered that a palladium catalyst with a high degree of phosphine ligand coordination (5 equiv of phosphine/mol Pd) was necessary to efficiently couple aryl siloxanes with 5-bromotropolone (4). In addition, the coupling approach has provided a direct comparison between siloxane and boronic acid coupling technologies that demonstrated that aryl siloxanes and boronic acids produce similar yields of highly functionalized biaryl products.
- Seganish, W. Michael,Handy, Christopher J.,DeShong, Philip
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p. 8948 - 8955
(2007/10/03)
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- Practical synthesis of biaryl colchicinoids containing 3′,4′- catechol ether-based A-rings via Suzuki cross-coupling with ligandless palladium in water
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Eight new biaryl colchicinoids containing 3′,4′-methylene or benzodioxy ether bridges were synthesized. The key synthetic step employed a ligandless, aqueous Suzuki cross-coupling reaction catalyzed by Pd(OAc) 2 with tetrabutylammonium bromide (TBAB) and potassium carbonate (K2CO3). The biaryl Suzuki products were typically formed in 5-30min and always in less than 1h.
- Deveau, Amy Morin,Macdonald, Timothy L.
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p. 803 - 807
(2007/10/03)
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- Syntheses and ipso-substitution reactions of some C-stannylated troponoids
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The C-stannylated troponoids (2)-(8) have been prepared and two of these shown to undergo palladium(0)-catalysed cross-coupling with bromobenzene to give the corresponding phenyl-substituted tropone. Compounds (3), (5) and (6)-(8) all react with electrophiles to give products of ipso-substitution.
- Banwell, Martin G.,Cameron, Jennifer M.,Collis, Maree P.,Gravatt, G. Lance
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p. 395 - 407
(2007/10/03)
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