新型手性配体的合成及其在沙美特罗关键中间体合成中的应用

New chiral ligand and its application in synthesis of a key intermediate of salmeterol

目的合成沙美特罗的关键手性中间体。方法设计合成新型手性配体单磺酰化1,2-双-(3,5-二甲基苯基)乙二胺,通过与金属铑配合生成手性催化剂,利用该催化剂催化沙美特罗的关键手性中间体的不对称氢转移反应。结果与结论新型手性配体具有良好的催化活性和对映体选择性,催化合成得到的沙美特罗中间体的对映体选择性的ee%值为91%。

Aim To develope a new asymmetric synthetic method of a key chiral intermediate for the synthesis of salmeterol. Methods A new chiral ligand, monosulfonated-1,2-（3, 5-dimethylphenyl） ethanediamine, was synthesized and applied in rhodium-catalyzed asymmetric synthesis of a key intermediate of salmeterol by transfer hydrogenation. Results and conclusion Higher yields and better enantioselectivities（up to 91% ee） can be obtained by use of the new chiral ligand in synthesis of intermediate of salmeterol.