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亚甲基二膦酸(Ⅰ)与氯化亚锡经冷冻干燥的无菌粉末,供~(?)钼——~(?)锝发生器配套,制备放射性~(?)锝亚甲基二膦酸盐注射液——骨显像剂,(简称MDP)。MDP 具有在血中的清除速度快,骨骼浓集度高,毒性低,不被肝脏所摄取等优点,故为目前较理想的骨骼显像剂。亚甲基二膦酸制备方法国内外有较多报道,现制备方法用异丙基磷酸酯,二溴甲烷加热回流反应20h 以上,再油泵减压除去低沸物,用盐酸水解得(?)。此制备方法反应时间长、收率低。我们选择了与文献类似的方法,经过反复实验,只将反应中生成的付产物2—溴代丙烷除去。改进后,工艺稳定,操作方便,反应时间缩短一半,收率也由原来的40%提高到85%。
Methylene diphosphonic acid (Ⅰ) with stannous chloride freeze-dried sterile powder for ~ (?) Molybdenum - ~? Tc generator to prepare radioactive ~ (~) technetium methylene bis Phosphate injection - bone imaging agent, (referred to as MDP). MDP has the advantages of fast clearance in the blood, high concentration of bone, low toxicity and ingestion by the liver, and is therefore an ideal bone imaging agent. Methylene diphosphonic acid preparation methods are more reported at home and abroad, the preparation method is the use of isopropyl phosphate, dibromomethane heating reflux reaction 20h above, and then remove the low-pressure oil pump decompression, hydrochloric acid hydrolysis (?). The preparation method has long reaction time and low yield. We chose a similar method to the literature, after repeated experiments, only the formation of the reaction product 2-bromopropane removed. After the improvement, the process is stable, the operation is convenient, the reaction time is shortened by half and the yield is increased from 40% to 85%.