| 摘要 |
In the compounds of the formula (IVa), (IVb), (IVc) or (IVd), R1 is C1-4alkyl or phenyl-C7-11alkyl. These compounds may be prepared by; a) reacting an arylamine of the formula R3R4CHNH2 (wherein R3 is H or C1-4alkyl and R4 is optionally substituted aryl) with a racemic alkoxyfuranone of the formula (II) (wherein R1 is as defined above) to produce the trans isomer (4R,5R) and (4S,5S) of the formulae (IIIa) and (IIIb) and separating the isomers by crystallization and optionally carrying out salification reactions, or when R3 is hydrogen, the isomers are resolved with an optically active acid; b) optionally subjecting a compound of formulae (IIIa) or (IIIb) in the presence of an acid to epimerization to obtain the cis isomers (4R,5S) or (4S,5R) of the formulae (IIIc) or (IIId); c) subjecting the trans isomer (4R,5R) or (4S,5S) of formulae (IIIa) or (IIIb) to hydrolysis to obtain the trans isomer (4R,5R) or (4S,5S) of compounds of formulae (IVa) or (IVb), which is then salified and/or protected; or subjecting the cis isomer of (4R,5S) or (4S,5R) of formulae (IIIc) or (IIId) to hydrolysis to obtain the cis isomer (4R,5S) or (4S,5R) of formulae (IVc) or (IVd) compounds, which is then salified and/or protected. The compounds of formula (IVa), (IVb), (IVc) or (IVd) may be used as inhibitors of interleukin-1beta converting enzyme.
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