- DIRECT C-H AMINATION AND AZA-ANNULATION
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In some aspects, the present disclosure provides methods of aminating an aromatic compound comprising reacting an aminating agent with an aromatic compound in the presence of a rhodium catalyst. In some embodiments, the methods may comprise aminating an aromatic compound which contains multiple different functional groups. The methods described herein may also be used to create bicyclic system comprising reacting an intramolecular aminating agent with an aromatic ring to obtain a second ring containing a nitrogen atom. In another aspect, the methods described herein may also be used to create a cyclic aliphatic cyclic/poly cyclic amine system comprising a reacting an intramolecular aminating agent by insertion into a C(sp3)-H bond.
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Paragraph 0132; 0262
(2019/06/07)
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- Tf2O-Promoted Intramolecular Schmidt Reaction of the ω-Azido Carboxylic Acids
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A designed Tf2O-promoted intramolecular Schmidt reaction of 2-substituted ω-azido carboxylic acids was demonstrated. Tf2O was used as an activation reagent for the carboxylic acid, and ω-azido anhydride was in situ generated, releasing a molecular TfOH, which acted as an acid promoter for the Schmidt process. A series of 2-substituted pyrrolidines was produced and acetylated for better purification. The strategy was also efficient for conversion of a 4-substituted ω-azido carboxylic acid to the tricyclic lactam.
- Wang, Xue-Juan,Su, Yan,Li, Rui,Gu, Peiming
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p. 5816 - 5824
(2018/05/14)
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- The insulin secretory action of novel polycyclic guanidines: Discovery through open innovation phenotypic screening, and exploration of structure-activity relationships
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We report the discovery of the glucose-dependent insulin secretogogue activity of a novel class of polycyclic guanidines through phenotypic screening as part of the Lilly Open Innovation Drug Discovery platform. Three compounds from the University of California, Irvine, 1-3, having the 3- arylhexahydropyrrolo[1,2-c]pyrimidin-1-amine scaffold acted as insulin secretagogues under high, but not low, glucose conditions. Exploration of the structure-activity relationship around the scaffold demonstrated the key role of the guanidine moiety, as well as the importance of two lipophilic regions, and led to the identification of 9h, which stimulated insulin secretion in isolated rat pancreatic islets in a glucose-dependent manner.
- Shaghafi, Michael B.,Barrett, David G.,Willard, Francis S.,Overman, Larry E.
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p. 1031 - 1036
(2014/03/21)
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- MODULATORS OF CENTRAL NERVOUS SYSTEM NEUROTRANSMITTERS
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Disclosed are agents having pharmacological activity against cellular receptors and intracellular singaling, particularly receptors and sigaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.
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Page/Page column 58
(2010/10/20)
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- THE PREPARATION OF "ELONGATED" NICOTINE ANALOGUES
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The preparation of four nicotine analogues having one or two additional methylene units between the N-methylpyrrolidinyl moiety and the aromatic ring are reported.Also prepared are the corresponding nornicotine and myosmine analogues.The course of the Spa
- Secor, Henry V.,Seeman, Jeffrey I.
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p. 1687 - 1698
(2007/10/02)
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