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

Eur. J. Org. Chem. 2018, 40, 5596-5604

DOI: 10.1002/ejoc.201800972

Homon A.; Hryshchuk O.; Trofymchuk S.; Michurin O.; Kuchkovska Y.; Radchenko D.; Grygorenko O.

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.

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

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