Abstract

Multiple bond-forming cascade transformations and one-pot procedures are valuable tools in organic synthesis and drug discovery. These atom-economical processes provide rapid access to natural product-like scaffolds from simple precursors. Herein, we report on ruthenium-catalyzed one-pot conversions of simple 1-alkenyl propargyl alcohols with cyclic 3-ketolactones and dienophiles. Thereby, structurally diverse fused polycycles and functionalized bicyclic structures are accessible from a common precursor with high selectivity. Some of the new drug-like molecules exhibit cytotoxic activity against KB cells.

Multiple bond-forming cascade transformations and one-pot procedures are valuable tools in organic synthesis and drug discovery. These atom-economical processes provide rapid access to natural product-like scaffolds from simple precursors. Herein, we report on ruthenium-catalyzed one-pot conversions of simple 1-alkenyl propargyl alcohols with cyclic 3-ketolactones and dienophiles. Thereby, structurally diverse fused polycycles and functionalized bicyclic structures are accessible from a common precursor with high selectivity. Some of the new drug-like molecules exhibit cytotoxic activity against KB cells.

中文翻译：

---

简单的炔丙基醇通过钌催化的级联反应和一锅法制备复杂的多环化合物

摘要

多重键形成级联转化和一锅法是有机合成和药物发现中有价值的工具。这些原子经济的方法使人们能够快速地从简单的前体中获得天然产物状的支架。在本文中，我们报道了钌催化的简单的1-烯基炔丙基醇与环3-酮内酯和亲二烯体的一锅转化。因此，可以从共同的前体以高选择性获得结构多样的稠合多环和官能化的双环结构。一些新的类药物分子对KB细胞表现出细胞毒活性。

多重键形成级联转化和一锅法是有机合成和药物发现中有价值的工具。这些原子经济的方法使人们能够快速地从简单的前体中获得天然产物状的支架。在本文中，我们报道了钌催化的简单的1-烯基炔丙基醇与环3-酮内酯和亲二烯体的一锅转化。因此，可以从共同的前体以高选择性获得结构多样的稠合多环和官能化的双环结构。一些新的类药物分子对KB细胞表现出细胞毒活性。