This paper discloses a method for preparing α‑ Chiral
amidine method. Through the in situ preparation of chiral
allylamine and alkenylimine, the asymmetric N‑ The heterogeneous
Claisen rearrangement method was successfully constructed α‑ Chiral
amidine. The reaction has the following advantages: (1) The
reaction conditions are very mild, the reaction can be carried out at
room temperature, and no equivalent strong base is required, which is more
environmentally friendly. (2) The one-pot two-
step method can eliminate the intermediate
processing steps for making chiral substrates, saving manpower and
material resources and reducing consumption. (3) It can simultaneously construct the chiral center and the
amidine functional group, with
atom economy and step economy. (4) The reaction yield is high, and the template product can be obtained with a total yield of 94% in two steps. The
chirality of
allylamine can also be stereospecifically transferred to the amidine, and the template product has 95% of (5) The substrate universality and functional group tolerance are good, such as cyano, tert-butyl, ester, methoxy, nitro, and
trifluoromethyl groups can all react, both ortho- and di-substitutions are active, and heteroaromatic compounds can also obtain the target product.