The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 7-Methoxy-1H-indole-3-carboxylic acid( cas:128717-77-1 ) is researched.Application of 128717-77-1.Cox, Brian; Duffy, James; Zdorichenko, Victor; Bellanger, Corentin; Hurcum, Jessica; Laleu, Benoit; Booker-Milburn, Kevin I.; Elliott, Luke D.; Robertson-Ralph, Michael; Swain, Christopher J.; Bishop, Stephen J.; Hallyburton, Irene; Anderson, Mark published the article 《Escaping from Flatland: Antimalarial Activity of sp3-Rich Bridged Pyrrolidine Derivatives》 about this compound( cas:128717-77-1 ) in ACS Medicinal Chemistry Letters. Keywords: pyrrolidine preparation antimalarial activity. Let’s learn more about this compound (cas:128717-77-1).
Synthetic photochem. to generate novel sp3-rich scaffolds and report the design, synthesis, and biol. testing of a diverse series of amides based on the 1-(amino-methyl)-2-benzyl-2-aza-bicyclo[2.1.1]hexane scaffold was utilized . Preliminary antimalarial screening of the library provided promising compounds with activity in the 1-5μM range with an enhanced hit rate. Further evaluation (solubility, drug metabolism and pharmacokinetics (DMPK), and toxicity) of a selected compound (9) suggested that this series represents an excellent opportunity for further optimization with the framework offering multiple opportunities for the addition of uniquely vectorally positioned extra functionality.
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Reference:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts