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Note | Regular issue | Vol 71, No. 2, 2007, pp.445-452
Published online, 26th December, 2006
DOI: 10.3987/COM-06-10941
Efficient Preparation of Medium Ring Oxygen Heterocycles

Atsuko Nishiguchi,* Tomomi Ikemoto, Tatsuya Ito, Shotaro Miura, and Kiminori Tomimatsu

*Chemical Development Laboratory, Takeda Chemical Industries, Ltd., 17-85 Jusohonmachi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan


We achieved efficient preparation of medium ring oxygen heterocycles (1), 1-benzoxepines and 1-benzoxocines, by applying intramolecular Claisen-type condensation in dialkyl carbonate with metal alcoholate. Furthermore, we accomplished the preparation of 2,3-dihydro-1-benzoxepin-4-carboxylate intermediate (1e) for orally active CCR5 antagonists by this method.