321596-56-9Relevant articles and documents
NOVEL ISOINDOLINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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Paragraph 0103; 0185; 0188, (2020/01/22)
Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α so as to effectively treat cancer and inflammatory diseases.
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases
Hecker, Scott J.,Reddy, K. Raja,Lomovskaya, Olga,Griffith, David C.,Rubio-Aparicio, Debora,Nelson, Kirk,Tsivkovski, Ruslan,Sun, Dongxu,Sabet, Mojgan,Tarazi, Ziad,Parkinson, Jonathan,Totrov, Maxim,Boyer, Serge H.,Glinka, Tomasz W.,Pemberton, Orville A.,Chen, Yu,Dudley, Michael N.
supporting information, p. 7491 - 7507 (2020/08/21)
Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory to inhibition by agents recently introduced. Most important among these are the class B (metallo) enzyme NDM-1 of Enterobacteriaceae and the class D (OXA) enzymes
Design and synthesis of florylpicoxamid, a fungicide derived from renewable raw materials
Babij, Nicholas R.,Choy, Nakyen,Cismesia, Megan A.,Couling, David J.,Hough, Nicole M.,Johnson, Peter L.,Klosin, Jerzy,Li, Xiaoyong,Lu, Yu,McCusker, Elizabeth O.,Meyer, Kevin G.,Renga, James M.,Rogers, Richard B.,Stockman, Kenneth E.,Webb, Nicola J.,Whiteker, Gregory T.,Zhu, Yuanming
, p. 6047 - 6054 (2020/10/18)
The design and synthesis of the broad-spectrum fungicide, florylpicoxamid, embodies multiple Green Chemistry principles. The active ingredient was strategically designed to deliver maximum biological activity and rapidly degrade after application to minimize its enviromental impact. Unlike many chiral crop protection chemicals, florylpicoxamid was purposely developed as a single stereoisomer to minimize the dose rate of this product in field applications and avoid any potential environmental burdens of its less active stereoisomers. Fortunately, the most efficacious stereoisomer of the natural product-inspired active ingredient can be derived from the natural antipodes of lactic acid and alanine. The principles of Green Chemistry were also used to improve the synthetic route originally developed for structure-activity relationship studies, resulting in a convergent stereoselective synthesis that is more sustainable and cost-effective. The streamlined 2ndgeneration route decreases the use of protecting groups and utilizes safer reaction solvents. Development of a novel synthetic sequence to the 2,3,4-trisubstituted pyridine motif from furfural further increased the renewable carbon content of the active ingredient to nearly 50%. Throughout process development, improved reaction conditions and industrially-preferred alternatives were identified to replace hazardous reagents for key transformations. In all, the holistic use of Green Chemistry principles in the design and synthesis of florylpicoxamid will provide farmers with a highly sustainable product for crop disease management.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0292, (2018/02/28)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
Fungicidal heterocyclic aromatic amides and their compositions, methods of use and preparation
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, (2015/09/28)
Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
Straightforward and efficient synthesis of 3-benzyloxy-4-bromopicolinate ester and 3-benzyloxy-5-bromopicolinate ester, common building blocks for pharmaceuticals and agrochemicals
Verdelet, Tristan,Mercey, Guillaume,Correa, Nobi,Jean, Ludovic,Renard, Pierre-Yves
experimental part, p. 8757 - 8762 (2011/11/29)
A practical and rapid preparation of 3-benzyloxy-4-bromo and 3-benzyloxy-5-bromopicolinate esters 10 and 16 was developed in four steps, respectively, in 38% and 31% overall yield. Then their viability as partners for cross-coupling reactions has been evaluated in Suzuki-Miyaura, Hartwig-Buchwald, and Sonogashira reactions to synthesize biologically relevant targets. The preparation of these two highly functionalizable pyridines 10 and 16 has been never described to date in the literature and could be used as common building block for the preparation of several biologically active compounds or agrochemical products.
Fungicidal heterocyclic aromatic amides and their compositions, methods of use and preparation
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, (2008/06/13)
A compound having the following formula: wherein R3and M are defined herein, and processes therewith.
