Department of Chemistry and Biochemistry, School of Green Chemistry and Engineering, The University of Toledo , 2801 West Bancroft Street, Toledo, Ohio 43606, United States.
Org Lett. 2017 Feb 17;19(4):930-933. doi: 10.1021/acs.orglett.7b00079. Epub 2017 Feb 8.
A convenient synthesis of a privileged pharmaceutical motif, thiazoline is accomplished. This reaction utilizes simple and readily available alkene and thioamide substrates in an intermolecular fashion via a simple one-pot procedure. A wide range of functional groups is tolerated, and the thiazoline product has been further utilized for the synthesis of the corresponding β-aminothiol and thiazole from routine hydrolysis and oxidation protocols.
一种方便的合成特权药物基序的方法,噻唑啉已经完成。该反应通过简单的一锅法,利用简单易得的烯烃和硫代酰胺底物进行分子间反应。该方法对各种官能团具有良好的耐受性,并且噻唑啉产物可进一步通过常规水解和氧化方法转化为相应的β-氨基硫醇和噻唑。