发明名称 NOVEL PROCESS FOR PRODUCING OPTICALLY ACTIVE 1,3-DISUBSTITUTED AZETIDINONE
摘要 PURPOSE:To obtain the subject compound useful as a synthetic intermediate for an antibacterial beta-lactam compound in high yield and stereo-selectivity by using a carboxylic acid derivative as a starting substance, subjecting the component to successive reactions and finally electrolyzing the reaction product. CONSTITUTION:The objective compound of formula VI can be produced by using a compound of formula I (R<3> is protected carboxyl) as a starting substance, reacting with formaldehyde or a substance having equivalent reactivity, reacting the reaction product with a compound of formula II (R<4> is lower alkyl), isomerizing the product to obtain a compound of formula III, reacting with an acid to acylate the primary alcohol and form a compound of formula IV (R<5> is acyl), introducing a hydroxy-protecting group, converting the resultant compound of formula V into a compound of formula R<2>-NH2 (R<2> is lower alkoxy) and electrolyzing the compound after cyclization reaction.
申请公布号 JPH03246274(A) 申请公布日期 1991.11.01
申请号 JP19900310831 申请日期 1990.11.15
申请人 FUJISAWA PHARMACEUT CO LTD 发明人 MURATA MASAYOSHI;CHIBA TOSHIYUKI;SHIRAI FUMIYUKI;WASHITSUKA KENICHI
分类号 C07D205/08 主分类号 C07D205/08
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