发明名称 PRODUCTION OF 2BETA-HALOGENO SUBSTITUTED METHYLPENICILLIN DERIVATIVE
摘要 PURPOSE:To obtain the title compound useful as an intermediate for beta-lactamase inhibitors and a cephalosporin based antibiotic in high purity and high yield, by reacting an azetidinone disulfide derivative with a hydrohalogenic acid in the presence of a nitrite, etc. CONSTITUTION:An azetidinone disulfide derivative expressed by formula I (R represents carboxyl-protecting group; R<1> and R<2> represent H, phthalimide, halogen or acylamino; R<3> represents nitrogen-containing heterocyclic group) [example; 2-oxo-4-(benzothiazol-2-yl)dithio-alpha-isopropenyl-1-azetidine acetic acid p-nitrobenzyl ester] is reacted with a hydrohalogenic acid (example; hydrochloric acid) in the presence of a nitrite (example; sodium nitrite) and/or an ester of nitrous acid to afford the aimed compound expressed by formula II (X represents halogen).
申请公布号 JPH01110689(A) 申请公布日期 1989.04.27
申请号 JP19870266943 申请日期 1987.10.21
申请人 TAIHO YAKUHIN KOGYO KK 发明人 TORII SHIGERU;TANAKA HIDEO;TANAKA MOTOAKI;YAMADA SHOZO;NAKAI AKIRA;OBAYASHI HISASHI
分类号 C07D499/87;A61K31/43;A61P31/04;C07D499/00;C07D499/44;C07D499/46;C07D499/80;C07D499/86;C07D499/897;C07D501/10 主分类号 C07D499/87
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