公开(公告)号：US5294712A

公开(公告)日：1994-03-15

申请号：US583296

申请日：1990-09-14

Applicant: Istvan Hermecz ,  Geza Keresturi ,  Lelle V. Debreczy ,  Agnes Horvath ,  Maria Balogh ,  Gabor Kovacs ,  Tamas Szuts ,  Peter Ritli ,  Judit Sipos ,  Aniko Pajor

Inventor： Istvan Hermecz ,  Geza Keresturi ,  Lelle V. Debreczy ,  Agnes Horvath ,  Maria Balogh ,  Gabor Kovacs ,  Tamas Szuts ,  Peter Ritli ,  Judit Sipos ,  Aniko Pajor

IPC: C07D215/56 ,  C07F5/02 ,  C07D401/04

CPC classification number: C07D215/56 ,  C07F5/022

Abstract: The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.

Abstract translation: 本发明涉及制备式I化合物（I）（其中R代表氢或甲基）及其药学上可接受的盐的新方法，其包括使式V化合物（V ）（其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或用于包含7-11个碳原子的芳族酰氧基）与式VI的胺（VI） （其中R具有与上述相同的含义）或其盐，并且如此获得的式VII（VII）化合物（其中R，R 1和R 2如上所述）在分离之后或在不分离之前进行水解，以及 如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。 式I的化合物是已知的抗菌剂。