METHOD FOR PRODUCING OPTICALLY ACTIVE SULFOXIDE DERIVATIVE
PROBLEM TO BE SOLVED: To provide a method for producing an optically active sulfoxide derivative having a CCR5 antagonistic action or its intermediate without side-reaction, e.g., racemization, Pummerer rearrangement. SOLUTION: The optically active compound (I) is produced by allowing a compound (II...
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Zusammenfassung: | PROBLEM TO BE SOLVED: To provide a method for producing an optically active sulfoxide derivative having a CCR5 antagonistic action or its intermediate without side-reaction, e.g., racemization, Pummerer rearrangement. SOLUTION: The optically active compound (I) is produced by allowing a compound (II) to react with a compound (III). In this case, these compounds (I), (II) and (III) are shown in the figure (wherein R1is H, an aliphatic hydrocarbon group, or an aromatic group; R2is a halogen, nitro, cyano, an alkyl, a cycloalkyl, hydroxy, thiol, amino, an acyl, carboxy or an aromatic group; R3is a 5- or 6-membered ring; R4is H, an alkyl, an alkoxy or a halogen; R5is H, a hydrocarbon group, a heterocyclic group, sulfonyl, carboxyl or an acyl; ring A is a benzene ring which may be substituted; X is a bond or a divalent group having 1-4 atoms constituting a straight chain part; (m) is an integer of 1-5; (n) is an integer of 0-3, (p) is an integer of 0-2 and *1means an asymmetric center). COPYRIGHT: (C)2004,JPO |
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