Abstract: The present application relates to a new method for synthesizing isophosphoramide nitrogen mustard (X-IPM) that is suitable for industrialized production, involves fewer types of solvents, and leads to stable products with high yield. This method is charazterized mainly by the batchwise addition of M (e.g., M is R3N with R being ethyl; i.e., M is triethylamine) and the specific post-reaction treatment, which make it possible for the reaction to fully proceed, lead to products with less impurities, high yield and relatively stable properties, and can lead to stable crystallized substances with specific crystal structures. The present application also relates to stable crystal forms of the isophosphoramide nitrogen mustard (X-IPM) prepared by the aforementioned method, and use of the same as reactants for the synthesis of aziridine structure-containing compounds.

Abstract: This invention relates to a process for preparing an intermediate of aminoimidazole carboxylate, a process for synthesizing aminoimidazole carboxylate and an HPLC method for determining purity. The process of preparing the intermediate of aminoimidazole carboxylate comprises subjecting a compound of formula I-2 and a formate as the reactants to a first-step reaction in a benzene solvent and at a temperature of ?5° C.?5° C., with the addition of a solution of sodium alkoxide in such a way that the temperature of the reaction solution is not higher than 5° C., to obtain the intermediate of aminoimidazole carboxylate or a mixture comprising a compound of formula I-3, i.e., the intermediate of aminoimidazole carboxylate.

Abstract: The present invention provides a preparation process of 1-N-methyl-2-nitro-5-hydroxymethylimidazole comprising using N,N?-carbonyldiimidazole and 1-N-methyl-2-aminoimidazole-5-carboxylic acid to react at 45˜65° C. for a period of time, and then cooling to 15˜25° C. for a period of time until the reaction is complete, and then reacting with a reducing agent to finally obtain 1-N-methyl-2-nitro-5-hydroxymethylimidazole. The present invention uses the relatively safe N,N?-carbonyldiimidazole to replace the highly toxic, strong irritating, strong corrosive, and environmentally demanding isobutyl chloroformate. It has the following advantages: CDI is a solid, non-irritating and non-corrosive, favorable for storage, transportation and environmental protection, low requirements on equipment, and less physical harm to operators; the reaction operation is simple and the post-treatment is simple.