Diverse functionalization of strong alkyl C–H bonds by undirected borylation. Rapid functionalization of multiple C–H bonds in unprotected alicyclic amines. Catalytic access to bridged sila-N-heterocycles from piperidines via cascade sp 3 and sp 2 C–Si bond formation. Palladium-catalysed transannular C–H functionalization of alicyclic amines. Ligand-controlled α- and β-arylation of acyclic N-Boc amines. Ligand-controlled β-selective C( sp 3)–H arylation of N-Boc-piperidines. Electrochemical aminoxyl-mediated α-cyanation of secondary piperidines for pharmaceutical building block diversification. Direct α-C–H bond functionalization of unprotected cyclic amines. Native functionality in triple catalytic cross-coupling: sp 3 C–H bonds as latent nucleophiles. Direct α-functionalization of saturated cyclic amines. A., Peschiulli, A., Lefevre, N., Meerpoel, L. Oxidative C–H/C–H coupling reactions between two (hetero)arenes.
Metal-free coupling of saturated heterocyclic sulfonylhydrazones with boronic acids. Lead-oriented synthesis: a new opportunity for synthetic chemistry. The 3-hydroxypiperidine skeleton: key element in natural product synthesis. The rise of fragment-based drug discovery. Natural toxins for use in pest management. Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among US FDA approved pharmaceuticals. The synthetic application of remote C–H activation within cyclic amines is exemplified by the synthesis of anisodamine via enantioselective hydroxylation of N-Boc-nortropinone. Substrate docking into molecular-dynamics-simulated structures of enzyme variants is shown to be useful for designing mutations to increase enantioselectivity by disfavouring binding poses leading to the unwanted enantiomer, and to increase enzymatic activity by disfavouring non-productive poses from ten or so variants per generation.
Different N-modifying groups provide product diversity at high enantioselectivity (up to 99% e.e.) from a panel of just 48 variants of P450 BM3. Here we report a combined substrate and enzyme engineering approach to achieve enantioselective functionalization of all unactivated C–H bonds of azepane, azocane, 7-azabicycloheptane and 8-azaspirodecane by cytochrome P450 BM3 (CYP102A1). Consequently, any such data, information, or opinions do not in any way represent a personal recommendation to any individual investor or any entities, whatever the type.Selective oxidation of ring C–H bonds is an attractive route to functionalized cyclic amines, which are versatile intermediates in drug synthesis and important fragment molecules in drug discovery. Nothing discussed or presented in Quantalytics constitutes a representation that any investment, investment strategy, or recommendation is suitable or appropriate to an investor's individual circumstances or otherwise constitutes a personal recommendation.ĭata, information, or opinions contained in Quantalytics in any form give no consideration to any particular individuals' investment needs or objectives, nor do they consider any individuals' financial condition. Quantalytics does not make any representations as to their accuracy or completeness. The data, information and opinions presented have been obtained or derived from sources believed by Quantalytics to be reliable. Any data, information, or opinions in Quantalytics in any form attributed to a third party represent Quantalytics’ interpretation of the data, information, or opinions provided by that third party either publicly or through a subscription service, and such use and interpretation have not been reviewed by the third party. Any data, information, or opinions expressed in any form may change without notice. Any forward looking estimates presented by Quantalytics may prove to be incorrect and not be realized. All investments and investment recommendations entail risks. Such data, information, or opinions are not an offer to sell or to buy, or a solicitation to buy or sell any securities. Any data, information, or opinions presented by Quantalytics are for general information purposes only. Quantalytics is not a registered investment adviser, brokerage firm, or investment company. Q.ai, LLC is a wholly owned subsidiary of Quantalytics Holdings, LLC (“Quantalytics”). Q.ai is the trade name of Quantalytics Holdings, LLC.
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