替米考星琥铂酸钠的制备和评价

Preparation and Evaluation of Tilmicosin Sodium Succinate

以4-二甲氨基吡啶(DMAP)为催化剂,通过替米考星与琥铂酸酐反应制备了替米考星琥铂酸酯.替米考星琥铂酸酯经与碳酸氢钠成盐反应,制备了替米考星琥铂酸酯钠盐.最佳工艺条件为:丙酮为溶剂,反应温度为56~57℃,反应时间为4 h,DMAP用量为替米考星用量的3%,n(替米考星)∶n(琥铂酸酐)=1∶2.4,n(替米考星琥铂酸酯)∶n(碳酸氢钠)=1∶2.在最佳工艺条件下,产物收率达90.3%.

Tilmicosin succinate is prepared by the reaction of tilmicosin with succinic anhydride using DMAP as catalyst.Telmicosin sodium succinate is prepared by the reaction of telmicosin succinate with sodium bicarbonate.The optimum conditions are as follows:acetone as solvent,reaction temperature 56-57℃,reaction time 4 h,the amount of DMAP is 3%of that of tilmicosin,n(tilmicosin)∶n(succinic anhydride)=1∶2.4,n(tilmicosin succinate)∶n(sodium bicarbonate)=1∶2.The yield of the product is 90.3%under the optimum conditions.