- Enantioselective Catalyst Systems from Copper(II) Triflate and BINOL–Silanediol
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Silanediol and copper catalysis are merged, for the first time, to create an enhanced Lewis acid catalyst system for enantioselective heterocycle functionalization. The promise of this silanediol and copper catalyst combination is demonstrated in the enantioselective addition of indoles to alkylidene malonates to give rise to the desirable adducts in excellent yield and high enantiomeric excess. From these studies, 1,1′-bi-2-naphthol (BINOL)-based silanediols emerge as one-of-a-kind cocatalysts. Their potential role in the reaction pathway is also discussed.
- Guan, Yong,Attard, Jonathan W.,Visco, Michael D.,Fisher, Thomas J.,Mattson, Anita E.
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supporting information
p. 7123 - 7127
(2018/05/08)
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- Organic photocatalysis for the radical couplings of boronic acid derivatives in batch and flow
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We report an acridium-based organic photocatalyst as an efficient replacement for iridium-based photocatalysts to oxidise boronic acid derivatives by a single electron process. Furthermore, we applied the developed catalytic system to the synthesis of four active pharmaceutical ingredients (APIs). A straightforward scale up approach using continuous flow photoreactors is also reported affording gram an hour throughput.
- Lima, Fabio,Grunenberg, Lars,Rahman, Husaini B. A.,Labes, Ricardo,Sedelmeier, Joerg,Ley, Steven V.
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supporting information
p. 5606 - 5609
(2018/06/04)
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- Protected amino hydroxy adamantane carboxylic acid and process for its preparation
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Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided. The provided compounds can be used for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
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Paragraph 0428; 0429
(2015/11/24)
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- Azepanone-based inhibitors of human cathepsin S: Optimization of selectivity via the P2 substituent
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A series of azepanone inhibitors of cathepsin S is described. Selectivity over both cathepsin K and cathepsin L was achieved by varying the P2 substituent. Ultimately, a balanced potency and selectivity profile was achieved in compound 39 possessing a 1-methylcyclohexyl alanine at P2 and nicotinamide as the P′ substituent. The cellular potency of selected analogs is also described.
- Kerns, Jeffrey K.,Nie, Hong,Bondinell, William,Widdowson, Katherine L.,Yamashita, Dennis S.,Rahman, Attiq,Podolin, Patricia L.,Carpenter, Donald C.,Jin, Qi,Riflade, Benoit,Dong, Xiaoyang,Nevins, Neysa,Keller, Paul M.,Mitchell, Laura,Tomaszek, Thaddeus
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scheme or table
p. 4409 - 4415
(2011/09/15)
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- Bronsted base-modulated Regioselective Pd-catalyzed intramolecular aerobic oxidative amination of alkenes: Formation of seven-membered amides and evidence for allylic C-H activation
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A novel palladium-catalyzed intramolecular aerobic oxidative allylic C-H amination of olefins has been developed. Bronsted base can modulate the regioselectivity, favoring the formation of 7-membered rings. Mechanistic studies using deuterium-labeled substrates as probes support a rate-determining allylic C-H activation/irreversible reductive elimination pathway.
- Wu, Liang,Qiu, Shuifa,Liu, Guosheng
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supporting information; scheme or table
p. 2707 - 2710
(2009/10/10)
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- Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability: Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α -Aminoacyl-L-cis-4,5-methanoprolinenitrile-Based Inhibitors
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A series of methanoprolinenitrile-containing dipeptide mimetics were synthesized and assayed as inhibitors of the N-terminal sequence-specific serine protease dipeptidyl peptidase IV (DPP-IV). The catalytic action of DPP-IV is the principle means of degradation of glucagon-like peptide-1, a key mediator of glucose-stimulated insulin secretion, and DPP-IV inhibition shows clinical benefit as a novel mechanism for treatment of type 2 diabetes. However, many of the reversible inhibitors to date suffer from chemical instability stemming from an amine to nitrile intramolecular cyclization. Installation of a cyclopropyl moiety at either the 3,4- or 4,5-position of traditional 2-cyanopyrrolidide proline mimetics led to compounds with potent inhibitory activity against the enzyme. Additionally, cis-4,5-methanoprolinenitriles with β-branching in the N-terminal amino acid provided enhanced chemical stability and high inhibitory potency. This class of inhibitors also exhibited the ability to suppress prandial glucose elevations after an oral glucose challenge in male Zucker rats.
- Magnin, David R.,Robl, Jeffrey A.,Sulsky, Richard B.,Augeri, David J.,Huang, Yanting,Simpkins, Ligaya M.,Taunk, Prakash C.,Betebenner, David A.,Robertson, James G.,Abboa-Offei, Benoni E.,Wang, Aiying,Cap, Michael,Xin, Li,Tao, Li,Sitkoff, Doree F.,Malley, Mary F.,Gougoutas, Jack Z.,Khanna, Ashish,Huang, Qi,Han, Song-Ping,Parker, Rex A.,Hamann, Lawrence G.
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p. 2587 - 2598
(2007/10/03)
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- Optically active pyridonecarboxylic acid derivatives
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N1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: STR1 These compounds have pate
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- Spiro compound
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The present invention relates to spiro compounds of general formula I: STR1 wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.
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