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2. 发明申请

WO02076515A2 METHOD OF PRODUCING 1-HYDROXY-1,1-DIPHOSPHONIC ACID COMPOUNDS 审中-公开
标题翻译：用于生产1-羟基-1,1-二膦酸
公开(公告)号：WO02076515A2
公开(公告)日：2002-10-03
申请号：PCT/EP0202676
申请日：2002-03-12
申请人： EUCRO EUROPE CONTRACT RES GMBH , BLUM HELMUT , GREB WOLFGANG , PUSTOVIT YURII , ROESCHENTHALER GERD-VOLKER
发明人： BLUM HELMUT , GREB WOLFGANG , PUSTOVIT YURII , ROESCHENTHALER GERD-VOLKER
IPC分类号： C07F7/18 , C07F9/38 , C07F9/40 , A61L9/02 , A23L1/22 , A61K31/465 , A63J23/02
CPC分类号： C07F9/386 , C07F9/3873 , C07F9/409
摘要： The invention relates to a method of producing the 1-hydroxy-1,1-diphosphonic acid compounds of general formula (I), and/or the pharmacologically acceptable salts thereof, in which formula R represents hydrogen, OH, NO2, Cl, F, Br, C1-C6 alkyl that may be substituted with halogen, amine and/or aminoalkyl, C1-6 alkoxy, aryl, heteroaryl, a group NR R , wherein R and R may be the same or different and represent hydrogen, C1-C6 alkyl, halogen-substituted alkyl, hydroxy-C1-alkyl; R represents hydrogen, halogen, amine that may be substituted, C1-C6 alkyl that may be substituted with halogen, amine and/or aminoalkyl, C1-C6 alkoxy, aryl, heteroaryl; Y represents O, S or NH; Z represents C1-C5 alkylene that may be substituted with amine groups, and m and n are 0 or 1, with the proviso that if n=1, m=1. According to the inventive method, a compound of formula (II), wherein R , R , Y, Z, m and n are defined as above, is reacted with a compound of the formula P(OSiR 3)3-pR p, wherein R represents a C1-C4 alkyl group, R represents a C1-C6 alkyloxy group, and p is 0, 1 or 2. The reaction product is hydrolyzed in a manner known pre se and is optionally converted to the corresponding salts.
摘要翻译：本发明提供了一种用于的1-羟基 - 1，制备具有I和/或它们的药理学上可接受的盐要求保护的通式，其中R <1>是氢，OH，NO 2，氯，氟，溴，C1 1二膦酸化合物 C6烷基，其也可以被卤素，氨基和/或氨基烷基，C 1-6烷氧基，芳基，杂芳基，基团NR <3> [R <4>，R <3>和R <取代的4- >相同或不同，是氢，C1-C6烷基，卤素 - 取代的烷基，羟基-C1-烷基，R <2>是氢，卤素，氨基可以被取代，C1-C6烷基，其也可以被卤素，氨基和/或氨基烷基，C1-C6-烷氧基，芳基，杂芳基取代，Y是O，S或NH; žC1-C5亚烷基，其可以通过氨基基团，m和被取代，n是0或1，条件是当n = 1，且m = 1，其中，所述式II的化合物，其中R <1 >，R <2>，Y，Z，m和n如上所定义，与具有式P的化合物（OSIR <5> 3）3-P - [R <6> 6，其中R <5>表示 C1-C4烷基，R <6>是一个C1-C6烷氧基，p是0，1或2转化水解，以已知的方式将反应产物和任选转化成盐。

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