A new and versatile synthesis of optically active alpha-fluoro-malonamides derivatives from enantiomerically pure 3-fluoro-2-azetidinones is described. A fluorinated retroamide isostere based on these alpha-fluoro-malonamide was introduced into a small peptidomimetic for use as an HIV-1 protease inhibitor.
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN
SATO, M
TAKAYAMA, K
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN
TAKAYAMA, K
SEKIGUCHI, K
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN
SEKIGUCHI, K
ABE, Y
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN
ABE, Y
FURUYA, T
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN
FURUYA, T
INUKAI, N
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN
INUKAI, N
KANEKO, C
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YAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPANYAMANOUCHI PHARMACEUT CO LTD, TSUKUBA RES LABS, TSUKUBA, IBARAKI 305, JAPAN