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1.发明公开PROCESS FOR PREPARING 3-(7-AMIDINO-2-NAPHTHYL)-2-PHENYLPROPIONIC ACID DERIVATIVES 失效用于制备3-（7-脒基-2-萘基）-2-苯基丙酸衍生物
公开(公告)号：EP0990646A4
公开(公告)日：2001-01-17
申请号：EP98921879
申请日：1998-05-29
申请人： DAIICHI SEIYAKU CO
发明人： MAKINO TORU , YOKOYAMA YUKIO
IPC分类号： C07D207/12
CPC分类号： C07D207/12
摘要： A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity (Japanese Patent Laid-Open No. 208946/1993), i.e., compounds represented by general formula (3) or salts thereof by the following reaction scheme (1), (2) and (3), wherein R1 represents H or an alkyl group; R2 represents H, an alkanoyl group, an alkoxycarbonyl group, an aralkyl group, an aralkyloxycarbonyl group or the like; and R3 represents H, an alkyl group, or an alkanoyl group.
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2.发明公开ENANTIOMERICALLY PURE SUBSTITUTED OXAAZA COMPOUNDS, SALTS OF THE SAME, AND PROCESSES FOR THE PREPARATION OF BOTH 有权对映异构的取代的OXAAZAVERBINDUNGEN及其盐和方法同时产生
公开(公告)号：EP1088825A4
公开(公告)日：2001-09-05
申请号：EP99957061
申请日：1999-06-16
申请人： DAIICHI SEIYAKU CO
发明人： OHTA NAOKI , MAKINO TORU , SHIMIZU SADAHIRO
IPC分类号： C07D207/14 , C07D498/04 , C07D498/10
CPC分类号： C07D207/14
摘要： A process for easily preparing compounds represented by general formula (Ia) which are useful as intermediates for the preparation of antimicrobial compounds, comprising reacting a compound represented by general formula (I) with a ketone and an optically active acid to form a salt of a compound represented by general formula (IIIa) with the optically active acid, converting the salt into a free base and hydrolyzing the free base wherein R1 is hydrogen, alkyl, aryl or aralkyl; and R2 is hydrogen, alkyl, aryl, aralkyl, acyl, alkyloxycarbonyl, aralkyloxycarbonyl or substituted sulfonyl, provided these groups may be further substituted.
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