Publications by authors named "Heng-Xian He"

Article Synopsis
  • Bicyclic scaffolds are important in drug discovery due to their ability to resemble benzene structures.
  • This study presents a novel method using a Lewis acid catalyst to facilitate a reaction between bicyclobutanes and diaziridines, yielding valuable azabicyclo[3.1.1]heptane compounds with high efficiency.
  • The research also successfully scaled up the process and introduced a chiral zinc-based catalyst to promote enantioselective synthesis, achieving significant optical purity.
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The absence of catalytic asymmetric methods for synthesizing chiral (hetero)bicyclo[n.1.1]alkanes has hindered their application in new drug discovery.

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The cycloaddition reaction involving bicyclo[1.1.0]butanes (BCBs) offers a versatile and efficient synthetic platform for producing C(sp)-rich rigid bridged ring scaffolds, which act as phenyl bioisosteres.

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