期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 77, 期 8, 页码 3820-3828出版社
AMER CHEMICAL SOC
DOI: 10.1021/jo3001595
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资金
- Merck Research Laboratories
A highly efficient synthesis of Vaniprevir (MK-7009) has been accomplished in nine linear steps and 55% overall yield. The key features of this synthesis include a cost-effective synthesis of the isoindoline subunit and efficient construction of the 20-membered macrocyclic core of Vaniprevir (MK-7009) utilizing ring-closing metathesis technology. A high-performing ring-closing metathesis protocol has been achieved by simultaneous slow addition of the ruthenium catalyst (0.2 mol %) and the diene substrate at a concentration of 0.13 M.
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