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Hetero-Diels–Alder Addition of Ethyl 2-Nitrosoacrylate to (Z)-Prop-1-enyl Ethers. Stereoselective Synthesis of a Precursor to Sacubitril
Synthesis ( IF 2.2 ) Pub Date : 2023-03-15 , DOI: 10.1055/a-2029-0015
Stavroula A Zisopoulou 1 , Thanos Andreou 2 , Theocharis Koftis 3 , John Gallos 4 , Christos Stathakis 5
中文翻译:
2-亚硝基丙烯酸乙酯与 (Z)-Prop-1-enyl Ethers 的杂-Diels-Alder 加成反应。沙库巴曲前体的立体选择性合成
更新日期:2023-03-16
Synthesis ( IF 2.2 ) Pub Date : 2023-03-15 , DOI: 10.1055/a-2029-0015
Stavroula A Zisopoulou 1 , Thanos Andreou 2 , Theocharis Koftis 3 , John Gallos 4 , Christos Stathakis 5
Affiliation
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A novel, conceptually distinct synthesis of a key precursor to sacubitril, an antihypertensive drug, is presented. The well-demonstrated hetero-Diels–Alder addition of in situ generated nitrosoalkenes to electron-rich enol ethers was engaged to establish the required functionalities with controllable relative stereochemistry. An asymmetric variant of the enol ether enabled access to the target molecule in enantiopure form.
中文翻译:
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2-亚硝基丙烯酸乙酯与 (Z)-Prop-1-enyl Ethers 的杂-Diels-Alder 加成反应。沙库巴曲前体的立体选择性合成
介绍了抗高血压药物沙库巴曲的关键前体的一种新颖的、概念上截然不同的合成方法。原位生成的亚硝基烯烃与富电子烯醇醚的杂 Diels-Alder 加成得到了充分证明,用于建立具有可控相对立体化学的所需功能。烯醇醚的不对称变体能够以对映体纯的形式接触目标分子。