米诺膦酸的磷酸化合成工艺改进

Improved Phosphorylation Process for Synthesis of Minodronic Acid

该文对米诺膦酸的磷酸化合成工艺进行了改进。该工艺以(咪唑并[1,2-a]吡啶-3-基)乙酸(2)为原料,甲磺酸做溶剂,仅使用三氯化磷为磷酸化试剂,不需亚磷酸和有机溶剂,产品收率82.4%,纯度99.82%;避免了非均相的反应状态,反应条件更加温和,成本降低。

In this study,the synthesis of minodronic acid by phosphorylation was improved.Started from(imidazolo[1,2-a]pyridin-3-yl)acetic acid(2),the phosphorylation was carried out only with phosphorus trichloride in methanesulfonic acid(as solvent).The product was obtained in a yield of 82.4%and a purity of 99.82%.The process did not use phosphorous acid and any organic solvent,so the heterogeneous reaction state was avoided.These reaction conditions were mild,and the production cost was reduced.