A stereoselective synthesis of (+)-L-733,060 from ethyl (R)-(+)-2,3-epoxypropanoate

作者：Prevost Sebastien; Phansavath Phannarath^*; Haddad Mansour

来源：Tetrahedron: Asymmetry , 2010, 21(1): 16-20.

DOI：10.1016/j.tetasy.2009.12.010

An asymmetric synthesis of neurokinin substance P receptor antagonist (+)-L-733,060 starting from enantiomerically pure ethyl (R)-(+)-2,3-epoxypropanoate (ethyl glycidate) is described The synthesis relies on a diastereoselective reductive animation, regioselective intramolecular epoxide opening, and in situ cyclization as the key steps.

• 出版日期2010-1-29