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Title:
4’-置換ヌクレオシド誘導体の立体選択的合成法
Document Type and Number:
Japanese Patent JP7025064
Kind Code:
B2
Abstract:
Current synthesis methods for 4'-substituted nucleoside derivatives include a step in which stereoisomers are produced and therefore have problems such as decreased yield and complication of a refinement step. Thus, a synthesis method has been sought that is simpler and does not produce stereoisomers. The present invention provides a synthesis method for a 4'-substituted nucleoside intermediate represented by formula (6), the method comprising the following steps 1 through 3: step 1 in which a compound of formula (3) is used as a starting raw material, and a nucleophile is made to act on the compound of formula (3) to obtain the compound of formula (4) in which a substituent group has been stereoselectively introduced; step 2 in which the compound of formula (4) is hydrolized to obtain the compound of formula (5); and step 3 in which the compound of formula (5) is held in acidic conditions to obtain the compound represented by formula (6). In the formulas, R1 indicates a protective group of a hydroxyl group, Me indicates a methyl group, and X indicates a substituent group.

Inventors:
Satoru Mugo
Tomoko Matsuura
Application Number:
JP2020535863A
Publication Date:
February 24, 2022
Filing Date:
August 08, 2019
Export Citation:
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Assignee:
Yamasa Shoyu Co., Ltd.
International Classes:
C07H15/04; C07H1/00; C07H9/04; C07H19/00; C07H19/067
Domestic Patent References:
JP2015523337A
JP2001335593A
JP11349596A
JP9328497A
Other References:
ANGEWANDTE CHEMIE , INTERNATIONAL EDITION,2015年,vol. 54, no. 24,pages 7185 - 7188
BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY,1993年,vol. 57, no. 9,pages 1433 - 1438