合成了一系列2-氧代-3(2 H)-苯并恶唑乙酸乙酯衍生物2。通过与氨,伯胺或肼反应,将这些化合物2分别转化为1-(2-羟苯基)-2,4-咪唑烷二酮衍生物4、5和6。这些新的乙内酰脲4,用三氯氧磷处理后,得到3 H -2-氧代咪唑并[2,1- b ]苯并恶唑衍生物9。通过丙烯酸乙酯与2-苯并恶唑酮(1a)的Michaël反应制备2-氧代-3(2 H)-苯并恶唑丙酸乙酯(10)。带10,在氨或烷基胺的存在下未观察到环状转化。
The present invention relates to 11,12 &ggr; lactone ketolides of formula (I) wherein R, R
1
, R
2
, R
3
are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R
1
, R
2
, R
3
are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.