10A-AZALIDE COMPOUND CROSSLINKED AT 10A- AND 12-POSITIONS
申请人:Sugimoto Tomohiro
公开号:US20110237784A1
公开(公告)日:2011-09-29
A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even
Hemophilus influenzae
, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
10A-AZALIDE COMPOUND CROSSLINKED AT POSITION-10A AND POSITION-12
申请人:Taisho Pharmaceutical Co. Ltd.
公开号:EP2177526A1
公开(公告)日:2010-04-21
A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even Hemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
The preparation and reactions of ortho-benzoquinone monohemiaminals are described. The oxidative dearomatization of phenols bearing amino alcohol groups induced N-cyclization to afford ortho-benzoquinone monohemiaminals. The N-cyclization stereoselectively affords the product when a chiral amino alcohol is used as the substituent. The chiral ortho-benzoquinone monohemiaminal undergoes stereoselective