Preparing edoxaban tosylate in formulating pharmaceutical composition, comprises reacting edoxaban with para-toluene sulfonic acid in alcohol solvent, and isolating edoxaban tosylate substantially free of N-oxide impurity
	BOPPANA D; SOMISETTI N R; NANDEPU H; NANDEPU V R
	2023-09-25
专利权人	METROCHEM API PVT LTD (METR-Non-standard)
申请日期	2023-09-25
专利号	IN202341064312-A
成果简介	NOVELTY - Preparing edoxaban tosylate (I) comprises (i) reacting edoxaban with para-toluene sulfonic acid in a suitable alcohol solvent containing less than 10 ppm of peroxide; and (ii) isolating edoxaban tosylate substantially free of N-oxide impurity; or (a) treating alcohol solvent containing more than 10 ppm of peroxide with a suitable base; (b) subjecting the solution to fractional distillation; (c) collecting the alcohol fraction containing less than 10 ppm of peroxide; (d) reacting edoxaban with para toluene sulfonic acid in the alcohol solvent; and (e) isolating the edoxaban tosylate substantially free of N-oxide impurity. USE - Method for preparing edoxaban tosylate in formulating pharmaceutical composition (claimed). ADVANTAGE - The method provides edoxaban tosylate with high yield, which has more than 99% purity by high-performance liquid chromatography, and is substantially free of N-oxide impurity. DETAILED DESCRIPTION - Preparing edoxaban tosylate of formula (I) comprises (i) reacting edoxaban with para-toluene sulfonic acid in a suitable alcohol solvent containing less than 10 ppm of peroxide; and (ii) isolating edoxaban tosylate substantially free of N-oxide impurity; or (a) treating alcohol solvent containing more than 10 ppm of peroxide with a suitable base; (b) subjecting the solution to fractional distillation; (c) collecting the alcohol fraction containing less than 10 ppm of peroxide; (d) reacting edoxaban with para toluene sulfonic acid in the alcohol solvent; and (e) isolating the edoxaban tosylate substantially free of N-oxide impurity. An INDEPENDENT CLAIM is included for edoxaban tosylate substantially free of N-oxide impurity, which is new.
IPC 分类号	A61K-031/444 ; A61P-007/02 ; C07D-213/75 ; C07D-513/04
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/20272
专题	中国科学院新疆生态与地理研究所
作者单位	METROCHEM API PVT LTD (METR-Non-standard)
推荐引用方式 GB/T 7714	BOPPANA D,SOMISETTI N R,NANDEPU H,et al. Preparing edoxaban tosylate in formulating pharmaceutical composition, comprises reacting edoxaban with para-toluene sulfonic acid in alcohol solvent, and isolating edoxaban tosylate substantially free of N-oxide impurity. IN202341064312-A[P]. 2023.

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