Centre for Synthesis and Chemical Biology (CSCB), Department of Pharmaceutical and Medicinal Chemistry, Royal College of Surgeons in Ireland, 123 St. Stephen's Green, Dublin 2, Ireland.
Chem Commun (Camb). 2012 Apr 21;48(32):3863-5. doi: 10.1039/c2cc30401e. Epub 2012 Mar 9.
Heavily substituted cyclopropane esters were prepared in high yields, complete diastereoselection and high (up to 96%) enantioselectivity. The reaction described herein entailed reacting 4-nitro-5-styrylisoxazoles, a class of cinnamate synthetic equivalent, with 2-bromomalonate esters under the catalysis of 5 mol% of a Cincona derived phase-transfer catalyst. The reaction allowed multi-gram preparation of desired products.
高收率、高对映选择性(高达 96%)、完全非对映选择性地制备了重取代的环丙烷酯。本文所描述的反应涉及在 Cincona 衍生的相转移催化剂的催化下,用 2-溴丙二酸酯与 4-硝基-5-苯乙烯基恶唑(一类肉桂酸合成等价物)反应。该反应允许多克制备所需产物。