Crystalline form of (r)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, preparation method therefor and use thereof

#The invention relates to (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, particularly to a crystalline form of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, preparation method and use thereof.

#4-hydroxy-2-oxo-1-pyrrolidineacetamide, its CAS No. is 62613-82-5, is a new generation of drug for improving cerebral metabolism that was first synthesized in 1974 by SmithKline Beecham Corporation, Italy and has been available on the market in 1987. 4-hydroxy-2-oxo-1-pyrrolidineacetamide is capable of promoting synthesis of phosphorylcholine and phosphoethanolamine, promoting cerebral metabolism, stimulating specific central nervous pathways through blood-brain barrier, and improving intelligence and memory. Studies have shown that its levorotatory form has a better curative effect of promoting brain and intelligence development. In recent years, it has been reported that its dextrorotatory form (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide has special biological activity in the field of sedation and anti-epilepsy, and has low toxicity and a broad range of pharmaceutical safety. Therefore, (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide is expected to become an alternative to the existing highly toxic anti-epileptic drugs.

#In order to effectively develop (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide into pharmaceutical products, a solid form that is easy to manufacture and has acceptable chemical and physical stability is required to facilitate its processing and circulating storage. The crystalline solid form is generally superior to the amorphous form in terms of enhancing the purity and stability of the compound. At present, there are few studies on preparation methods and crystalline forms of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, and no crystalline form of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide has been disclosed.

#FIG. 1 is a powder diffraction pattern of the crystalline form I of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide.

#When describing the compound, crystalline form, uses, compositions and methods of the invention, the following terms have the following meanings, unless otherwise stated.

#The term “therapeutically effective amount” means an amount that is sufficient to effect treatment when the amount is administered to a patient in need of treatment. As used herein, the term “treating” means treating a disease, illness or medical condition of a patient, for example, mammal (particularly human), comprising:

#(a) preventing the occurrence of the disease, illness or medical condition, namely preventive treatment of the patient;