Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinical Pharmacology, the NMPA and State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.
Chem Commun (Camb). 2022 Aug 16;58(66):9222-9225. doi: 10.1039/d2cc03007a.
An efficient Michael/aldol/ring-opening cascade reaction of cyclobutanones with chalcones has been developed. This protocol employs inexpensive potassium -butoxide (KOBu) as a promoter and enables an efficient synthesis of densely substituted cyclohex-3-ene-carboxylic acids in high yields with high diastereoselectivities, which are difficult to prepare through conventional approaches. The significant advantages of this methodology include transition-metal-free conditions, readily available starting materials, wide scope and high atom economy.
已开发出一种高效的环丁酮与查耳酮的迈克尔/aldol/开环级联反应。该方案采用廉价的碳酸钾(KOBu)作为促进剂,可高效合成高收率、高非对映选择性的稠取代环己-3-烯-羧酸,这在常规方法中难以制备。该方法的显著优点包括无过渡金属条件、易得的起始原料、广泛的适用范围和高原子经济性。