| abstract |
The invention discloses a preparation method of minodronic acid hydrate, which comprises: first protecting the compound (VII) on the keto group to obtain the compound (VI), and then performing nucleophilic reaction on the compound (VI) and 2-aminopyridine Substitution reaction to obtain compound (Ⅴ), compound (Ⅴ) undergoes cyclization reaction after deketo protection to obtain compound (Ⅳ); compound (Ⅳ) is hydrolyzed to obtain compound (Ⅲ), and compound (Ⅲ) is double phosphorylated Compound (II) is obtained after compound (II), and minodronic acid hydrate (I) is obtained after recrystallization of compound (II); the starting material source of the synthetic route of the present invention is sufficient, the cost is low, and the reagents used in the reaction process are environmentally friendly and industrial The production is safe, and the reaction conditions are mild, the operation is convenient, the side reaction is few, the post-treatment is simple, no special or complex reaction equipment is needed, and the industrial production is easy. |