反应详情

Scheme 4 provides an example of an embodiment of the process shown in Scheme 3. In this particular embodiment, the chiral diamine is (−)-sparteine, the organometallic compound is an organolithium compound, and more concretely it is s-BuLi, the solvent is Et2O, the strained cyclic ether is the epoxide ethylene oxide, the Lewis acid is BF3, provided as BF3.Et2O, m=1, and n=3. A compound of formula (Ia) in Scheme 4 can be characterized as being the enantiomer (+)-(R) because it is obtained in an ee of at least 80%, and in some embodiments about 82%. A compound of formula (Ia) was obtained in embodiments of this invention with a yield of about 83% and ee of about 82%.

1. customScheme 4 provides an example of an embodiment of the process