The invention discloses a method for
enantioselective synthesis of NH-
aziridine, which comprises the following steps: in the presence of a chiral
phosphoric acid catalyst, reacting alpha-cyano heterocyclic conjugated olefin as shown in a formula (I) with N-acyloxyhydroxylamine in an
organic solvent to obtain NH-
aziridine as shown in a formula (II), according to the present invention, the method can be smoothly performed in the
inert organic solvent at the temperature of-40-25 DEG C, the substrate can suitably cover
pyridine,
quinoline,
benzimidazole,
benzothiazole,
benzoxazole and other N-heteroaromatic rings, the product yield is high, and the
enantiomeric excess (ee) can be up to 99%. Inorganic additives (such as
magnesium oxide) may be optionally added during the reaction to increase yield on individual substrates without affecting enantioselectivity. The method avoids the traditional multi-step sequence of
nitrogen protection first and then deprotection, and has the advantages of economical steps, mild conditions, feasible amplification and the like.