Humanes Marcos, Sans-Panadés Ester, Virumbrales Cintia, Milián Ana, Sanz Roberto, García-García Patricia, Fernández-Rodríguez Manuel A
Departamento de Química Orgánica y Química Inorgánica, Instituto de Investigación Química "Andrés M. del Río" (IQAR), Universidad de Alcalá (IRYCIS), 28805 Alcalá de Henares, Madrid, Spain.
Área de Química Orgánica, Departamento de Química, Facultad de Ciencias, Universidad de Burgos, Pza. Misael Bañuelos s/n, 09001 Burgos, Spain.
Org Lett. 2024 Aug 9;26(31):6568-6573. doi: 10.1021/acs.orglett.4c02092. Epub 2024 Jul 28.
A selective, metal-free synthesis of boron-functionalized indenes and benzofulvenes via BCl-mediated cyclization of -alkynylstyrenes is described. The method allows precise control over product formation by adjusting reaction conditions. These borylated products were utilized in diverse C-B bond derivatizations and in the total synthesis of Sulindac, a nonsteroidal anti-inflammatory drug, demonstrating the versatility and practicality of the developed methodology for synthetic applications.
描述了一种通过硼氯介导的炔基苯乙烯环化反应选择性地、无金属合成硼官能化茚和苯并富烯的方法。该方法通过调整反应条件能够精确控制产物的形成。这些硼化产物被用于多种碳硼键衍生化反应以及非甾体抗炎药舒林酸的全合成中,证明了所开发方法在合成应用中的多功能性和实用性。