Synthesis of Macrocyclic Enediynes by Twofold C-Alkylation

Abstract
The alkylation of malonate derivatives with the new bis-electrophile 4 gave 18-membered macrocyclic enediynes 6a-c by a 2:2 alkylation process. The thermal stability of the bis(enediyne) 6a was investigated by differential scanning calorimetry. X-ray structure analyses revealed chair and twisted conformations of the macrocycles 6b and 6c in the crystal.

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