2-氧杂双环[2.1.1]己烷：合成、性质及作为邻位和间位苯生物电子等排体的验证
2-Oxabicyclo[2.1.1]hexanes: Synthesis, Properties, and Validation as Bioisosteres of ortho- and meta-Benzenes.
作者信息
Levterov Vadym V, Panasiuk Yaroslav, Shablykin Oleh, Stashkevych Oleksandr, Sahun Kateryna, Rassokhin Artur, Sadkova Iryna, Lesyk Dmytro, Anisiforova Anna, Holota Yuliia, Borysko Petro, Bodenchuk Iryna, Voloshchuk Nataliya M, Mykhailiuk Pavel K
机构信息
Enamine Ltd, Winston Churchill Str. 78, 02094, Kyiv, Ukraine.
V. P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry NAS of Ukraine, Academician Kukhar Str. 1, 02094, Kyiv, Ukraine.
出版信息
Angew Chem Int Ed Engl. 2024 May 6;63(19):e202319831. doi: 10.1002/anie.202319831. Epub 2024 Apr 3.
We have developed a general and practical approach towards 2-oxabicyclo[2.1.1]hexanes with two and three exit vectors via an iodocyclization reaction. The obtained compounds have been easily converted into the corresponding building blocks for use in medicinal chemistry. 2-Oxabicyclo[2.1.1]hexanes have been incorporated into the structure of five drugs and three agrochemicals, and validated biologically as bioisosteres of ortho- and meta-benzenes.
我们通过碘环化反应开发了一种通用且实用的方法来合成具有两个和三个离去基团的2-氧杂双环[2.1.1]己烷。所得到的化合物已很容易地转化为用于药物化学的相应结构单元。2-氧杂双环[2.1.1]己烷已被纳入五种药物和三种农用化学品的结构中，并作为邻位和间位苯的生物电子等排体进行了生物学验证。
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