Efficient synthesis of CCR5 antagonist, 2,3-dihydro-1-benzothiepine derivatives by improved intramolecular Claisen type reaction using dialkylcarbonate |
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Authors: | Tomomi Ikemoto Tatsuya Ito Atsuko Nishiguchi Kiminori Tomimatsu |
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Affiliation: | Chemical Development Laboratories, Takeda Pharmaceutical Company Limited, 2-17-85 Jusohonmachi, Yodogawa-ku, Osaka 532-8686, Japan |
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Abstract: | The efficient synthesis of 2,3-dihydro-1-benzothiepine derivatives 4 has been developed. The intramolecular Claisen type reaction of the new products, 4-(o-formylphenylthio)butyrate 9, with alcoholate in dialkylcarbonate as a solvent afforded 4 in good yields. According to this new procedure, we have accomplished the practical preparation of CCR5 antagonist 1 as a candidate for oral HIV-1 therapy. |
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Keywords: | 2,3-Dihydro-1-benzothiepine Claisen type condensation Dialkylcarbonate CCR5 antagonist |
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