A New Modular Indole Synthesis. Construction of the Highly Strained CDEF Parent Tetracycle of Nodulisporic Acids A and B

Construction of the highly strained CDEF parent tetracycle, a structural motif found only in the potent ectoparasiticidal agents (+)-nodulisporic
acids A and B and related congeners, has been achieved via a new modular indole synthesis, exploiting a sequential Stille cross-coupling/Buchwald−Hartwig union/cyclization tactic. The new indole synthesis holds the promise of rapid assembly of diverse, highly substituted
indoles possessing uncommon substitution patterns.

高张力CDEF母四环骨架作为仅存在于强效体外杀虫药剂(+)-诺杜斯波尔酸A、B及相关同系物中的结构基元，已通过新型模块化吲哚合成法实现构建，该方法采用连续斯蒂尔交叉偶联（Stille cross-coupling）/布赫瓦尔德-哈特维希偶联（Buchwald−Hartwig union）/环化策略。此新型吲哚合成法有望快速构建多样化、高度取代且带有罕见取代模式的吲哚类化合物。