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filingDate 1998-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2001-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2001521019-A
titleOfInvention Optically active intermediates for preparing optically active substituted oximes, hydrazones and olefins useful as neurokinin antagonists
abstract (57) Abstract: Intermediates having formula (A) and (B) are disclosed: wherein, B 1 is -CH 2 OH or -CH 2 OR P, and R P is a protecting group of the alcohol in it; a is 1, 2 or 3; T I is an -OH or (C); Q I is phenyl having 1-3 substituents, naphthyl or heteroaryl; R a and R c is the same and is H, or is selected from an alkyl, cycloalkyl and aryl group, where the group is required with one or more substituents selected from alkyl, cycloalkyl, aryl or -OH Or R a and R c together with the C—N—C chain to which they are attached form a 5- to 7-membered ring; R b and R d are identical; And H, or alkyl, cycloalkyl and Selected from a reel group, which group is optionally substituted with one or more substituents selected from alkyl, cycloalkyl, aryl or -OH; and D is a nitrogen compound reacting with s-butyllithium. In this case, it is an orientation group capable of directing α-lithiation to the nitrogen atom of the nitrogen compound having D as a substituent bonded to the nitrogen atom. This intermediate has optically active substituted oximes, hydrazones and olefins in which the R enantiomer has an enantiomeric excess of greater than 85%, preferably greater than 95%, relative to the corresponding S enantiomer and is useful as a neurokinin antagonist It is useful for preparing Embedded image
priorityDate 1997-10-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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