Synthesis of 3‐Azabicyclo[3.2.0]heptane‐Derived Building Blocks via [3+2] Cycloaddition

An efficient approach to synthesis of various substituted 3‐azabicyclo[3.2.0]heptane‐derived building blocks based on [3+2] cycloaddition of cyclobut‐1‐eneraboxylic acid ester and in situ generated azomethine ylide was developed and applied on multigram scale. The utility of 1,3‐disubstituted 3‐azabicyclo[3.2.0]heptane scaffold was demonstrated by additional structural analysis using exit vector plot (EVP) tool, and tested in parallel synthesis of compound library.