公开(公告)号：US07064198B2

公开(公告)日：2006-06-20

申请号：US10468584

申请日：2001-07-25

申请人： Vinod Kumar Kansal ,  Sunil Gurudatt Bhat ,  Tanguturi Venkata Marutikumar ,  Yuvaraj Atmaram Chavan ,  Ramanathan Sankaran

发明人： Vinod Kumar Kansal ,  Sunil Gurudatt Bhat ,  Tanguturi Venkata Marutikumar ,  Yuvaraj Atmaram Chavan ,  Ramanathan Sankaran

IPC分类号： C07D501/34 ,  C07D501/04

CPC分类号： C07D501/00

摘要： A process for preparation of cefuroxime axetil of formula (I) of at least 96% purity and substantially free of analogous Δ2-isomer of formula (II) and other impurities. The process comprises reacting cefuroxime acid of formula (III) with (R,S)-1-acetoxyethyl bromide of formula (IV), and a Group I or II metal carbonate in the presence of a compound of formula (V), MmHnPqOr  (V) wherein M is Group I or II metal; m is 1, 2, 3; n is 0, 1, 2, or 4; q is 1 or 2; r is 4, 7 or 8; in the presence of a C1-4 alcohol and a polar tertiary amide solvent selected from N,N-dimethylacetamide, N,N-dimethylformamide, N,N-dimetheylpropionamide, N,N-diethylacetamide, N,N-diethylformamide and N,N-diethylpropionamide at a temperature ranging from about −30 to +30° C. and subjecting the product thus obtained to a desired step of purification.

摘要翻译： 制备具有至少96％纯度且基本上不含式（II）的类似的三异构体和其它杂质的式（I）头孢呋辛酯的方法。 该方法包括使式（III）的头孢呋辛酸与式（IV）的（R，S）-1-乙酰氧基乙基溴和I或II族金属碳酸盐在式（Ⅴ）化合物存在下反应， in-line-formula description =“In-line Formulas”end =“lead”？> M＆lt;＆lt;＆lt; n＆gt;＆lt;＆lt;＆lt; （V）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中M是I或II族金属; m为1,2,3; n为0,1,2或4; q为1或2; r为4,7或8; 在C 1-4醇和极性叔胺溶剂的存在下，选自N，N-二甲基乙酰胺，N，N-二甲基甲酰胺，N，N-二甲酰基丙酰胺，N，N-二乙基乙酰胺，N ，N-二乙基甲酰胺和N，N-二乙基丙酰胺，温度范围为约-30至+ 30℃，并将所得产物经过所需的纯化步骤。