Abstract
An approach to the synthesis of conformationally restricted saturated
heterocyclic sulfonyl chlorides is described. Being guided by the
principle of diversity-oriented conformational restriction, a mini-library
of saturated heterocyclic sulfonyl chlorides was designed and synthesized.
The library consists of nine members that are derivatives of azetidine,
pyrrolidine, and piperidine. These compounds were prepared in 19-88% total
yields on multigram scale starting from the corresponding Cbz-protected amino
alcohols.
Key words
sulfonyl chlorides - nitrogen heterocycles - molecular rigidity - libraries - conformational restriction
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