A practical and efficient procedure for the enantioselective synthesis of mexiletine analogues using 10% of a novel spiroborate ester as chirality transfer agent is presented. A variety of mexiletine analogues were prepared with excellent enantioselectivities (91-97% ee) in good yield from readily available starting materials. The developed methodology was also successfully applied for the synthesis of novel β-amino ethers containing thiophenyl and pyridyl fragments.
                            本文介绍了一种实用高效的方法,使用10%的新型螺环
硼酸酯作为手性转移剂,对
美西律啶类似物进行对映选择性合成。采用易得的起始材料,制备出多种
美西律啶类似物,其对映选择性良好(91-97% ee),收率较高。该方法还成功地应用于合成含有
噻吩基和
吡啶基的新型β-
氨基醚。