Institute of Microbial Chemistry, Tokyo, Japan.
Angew Chem Int Ed Engl. 2012 Aug 20;51(34):8551-4. doi: 10.1002/anie.201204365. Epub 2012 Jul 16.
Softly does it: The title reaction proceeded under proton transfer conditions with a catalyst prepared from commercially available reagents to afford the desired product in high enantioselectivity. The reaction was compatible with a free amino group, thus allowing for expeditious access to enantiomerically enriched 1,5-benzothiazepines, which are important chemical entities in medicinal chemistry.
该标题反应在质子转移条件下进行,使用市售试剂制备的催化剂可高对映选择性地得到所需产物。该反应与游离氨基相容,因此可快速获得对映体富集的 1,5-苯并硫氮杂卓,这在药物化学中是重要的化学实体。