吡嗪
区域选择性
化学
吡唑
取代基
哌嗪
组合化学
双功能
脚手架
合成子
立体选择性
立体化学
有机化学
计算机科学
催化作用
数据库
作者
Vladimir I. Bozhanov,Dmytro P. Bohdan,Oleksandr V. Borysov,A. V. Silin,Oleg V. Zaremba,Mykola M. Avramenko,Dmitriy M. Volochnyuk,Sergey V. Ryabukhin,Konstantin S. Gavrilenko
标识
DOI:10.1002/slct.202104287
摘要
Abstract A set of building blocks based on the 4,5,6,7‐tetrahydro‐pyrazolo[1,5‐a]pyrazine scaffold is synthesized in a multigram scale in a cost‐efficient manner. The possibility of the introduction of different substituents, neutral or functionalized in different positions of pyrazole and/or piperazine rings, is shown. The efficacy of using NH‐pyrazole carbonic acids as a key intermediate of the process is demonstrated. The regioselectivity for direct insertion of the substituent to the 4,5,6,7‐tetrahydro‐pyrazolo[1,5‐a]pyrazine core is discussed. The synthetic perspectives for using the functionalized 4,5,6,7‐tetrahydro‐pyrazolo[1,5‐a]pyrazine as a bifunctional scaffold is discussed. The utilizing of building blocks obtained for the different region‐ and/or stereoselective synthesis, including sole transformations or modifications of functional groups, is demonstrated. The advantages of the proposed approach are proven compared with the other known methodologies.
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