A Building Block Approach for the Total Synthesis of YM-385781.
A Building Block Approach for the Total Synthesis of YM-385781.
复制标题
YM-385781 全合成的构建模块方法。
DOI：
10.1002/ejoc.202300365
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发表时间：
2023
影响因子：
2.8
通讯作者：
Moeller,KevinD
中科院分区：
文献类型：
--
作者：
Zhu,Yu;Liu,Siyue;Zigmond,Johnny;Kaltenbronn,KevinM;Blumer,KendallJ;Moeller,KevinD
YM-254890和FR 900359是Gq/11-信号通路的强效和选择性抑制剂。因此，它们一直是合成和生物学研究的有吸引力的靶标。然而，尽管做出了这些努力，但允许快速构建各种非天然和标记类似物并增加可用的这些类似物的量的分子的通用合成方法仍然难以捉摸。我们在这里报告一个收敛的积木方法的分子，可以解决这一挑战。
YM‐254890 and FR900359 are potent and selective inhibitors of the Gq/11‐signaling pathway. As such, they have been attractive targets for both synthesis and biological studies. Yet in spite of this effort, a versatile synthetic approach to the molecules that allows for the rapid construction of a variety of non‐natural and labelled analogs and an increase in the amount of those analogs available remains elusive. We report here a convergent building block approach to the molecules that can solve this challenge.