公开(公告)号：US06384212B1

公开(公告)日：2002-05-07

申请号：US09564980

申请日：2000-05-04

申请人： Dae-chul Yoon ,  Seung Won Yoo ,  Dong Gyun Shin ,  Myoung Ki Lee ,  Mi Soon Park ,  Yoon Seok Lee ,  Yoon Seok Song ,  Ju Cheol Lee ,  Sang Mi Oh

发明人： Dae-chul Yoon ,  Seung Won Yoo ,  Dong Gyun Shin ,  Myoung Ki Lee ,  Mi Soon Park ,  Yoon Seok Lee ,  Yoon Seok Song ,  Ju Cheol Lee ,  Sang Mi Oh

IPC分类号： C07D50124

CPC分类号： C07D501/00

摘要： The present invention relates to a new, simple, and easy process for preparing cephalosporin antibiotics of the following formula (I), such as ceftazidime and cefixime. The process comprises acylating a 7-amino cephalosporanic acid derivative of the following formula (III) with a crystalline aminothiazole compound of the following formula (II): wherein R1 and R2 are the same or different and independently represent H, a C1-4 alkyl or C3-5 cycloalkyl group, R4 represents acetoxymethyl, methylpyridine, or vinyl, X represents chlorine or bromine, and the acid in the acid addition salt represents an inorganic acid, such as hydrochloric acid, or an organic acid, such as formic acid or acetic acid.

摘要翻译： 本发明涉及用于制备下列通式（I）的头孢菌素抗生素的新的，简单的和容易的方法，例如头孢他啶和头孢克肟。 该方法包括用下式（II）的结晶氨基噻唑化合物酰化下式（III）的7-氨基头孢菌酸衍生物：其中R 1和R 2相同或不同并且独立地代表H，C 1-4烷基 或C3-5环烷基，R4表示乙酰氧基甲基，甲基吡啶或乙烯基，X表示氯或溴，酸加成盐中的酸表示无机酸，如盐酸或有机酸，如甲酸或 醋酸。

公开(公告)号：US06277996B1

公开(公告)日：2001-08-21

申请号：US09564979

申请日：2000-05-04

申请人： Dae-chul Yoon ,  Seung-won Yoo ,  Dong Gyun Shin ,  Myoung Ki Lee ,  Mi Soon Park ,  Yoon Seok Lee ,  Yoon Seok Song

发明人： Dae-chul Yoon ,  Seung-won Yoo ,  Dong Gyun Shin ,  Myoung Ki Lee ,  Mi Soon Park ,  Yoon Seok Lee ,  Yoon Seok Song

IPC分类号： C07D27738

CPC分类号： C07D277/40 ,  Y02P20/55

摘要： The present invention relates to a new crystalline aminothiazole derivative represented by the following formula (I) which is very useful for the preparation of cephalosporin antibiotics, including ceftazidime and cefixime, etc: wherein R1 and R2 are the same or different and independently represent H, an alkyl group of 1 to 4 carbon atoms, or a cycloalkyl group of 3 to 5 carbon atoms, X represents chlorine or bromine, and the acid in the acid addition salt represents an inorganic acid, such as hydrochloric acid, hydrobromic acid, sulfuric acid, or perchloric acid, or an organic acid, such as formic acid, acetic acid, trifluoroacetic acid, propionic acid, methanesulfonic acid, or benzenesulfonic acid.

摘要翻译： 本发明涉及一种非常适用于头孢菌素和头孢克肟等头孢菌素抗生素非常有用的新型结晶氨基噻唑衍生物，其中R1和R2相同或不同，独立地代表H， 1〜4个碳原子的烷基或3〜5个碳原子的环烷基，X表示氯或溴，酸加成盐中的酸表示无机酸，如盐酸，氢溴酸，硫酸 或高氯酸，或有机酸如甲酸，乙酸，三氟乙酸，丙酸，甲磺酸或苯磺酸。