886985-48-4Relevant academic research and scientific papers
Benzobutyrolactone derivatives, synthetic method and application thereof in preparation of bactericides
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Paragraph 0049; 0050; 0051, (2018/04/03)
The invention discloses benzobutyrolactone derivatives, a synthetic method and application thereof in preparation of bactericides. The method comprises the following steps: taking sesquiterpene lactone pharmacophore alpha-methylene-gamma-butyrolactone as a lead compound, integrating benzofuranone pharmacophore, modifying at an alpha-methylene position, and performing directional derivative synthesis to obtain a series of alpha-alkenylene benzobutyrolactone compounds. The antibacterial activities of the compounds are determined, and two high-activity compounds with excellent industrialization development prospects are synthesized on the structure-effect basis. The compounds are used for controlling plant diseases caused by pathogenic bacteria such as wheat powdery mildew, wheat scab, take-all disease of wheat, wheat sharp eyespot, corn northern leaf blight, rice sheath blight disease, rice blast, cotton damping-off, phytoph-thora capsici leonian, botrytis cinerea, tomato leaf mould, tomato early/late blight, cucumber anthracnose, fusarium wilt of cucumber, sclerotinia rot of colza and the like.
Synthesis of Oxindoles and Benzofuranones via Oxidation of 2-Heterocyclic BMIDAs
Seath, Ciaran P.,Fyfe, James W. B.,Molloy, John J.,Watson, Allan J. B.
, p. 891 - 898 (2017/02/15)
The synthesis of functionalized oxindoles and benzofuranones via oxidation of 2-BMIDA indoles and benzofurans, respectively, is described. Interconversion of boron species (BMIDA→BF3K) was necessary to enable oxidation and overcome boronic acid stability issues associated with a difficult BMIDA hydrolysis. Overall, a robust process was developed that allowed access to a small library of oxindole and benzofuranone products and facilitated the step-efficient synthesis of biologically active compounds containing the oxindole pharmaco-phore.
