Preparing cortexolone 17 alpha-propionate, for treating acne vulgaris in patients involves hydrolyzing an ortho-ester in the presence of at least one acid selected from formic acid, ascorbic acid, benzoic acid, aluminium trichloride and its mixtures to obtain cortexolone 17alpha-propionate
	KATRAGADDA V R; KUNDETI P; RAVURI S; KOLLA R
	2023-09-12
专利权人	PULSE PHARM PVT LTD (PULS-Non-standard)
申请日期	2023-09-12
专利号	IN202341061366-A
成果简介	NOVELTY - Preparing cortexolone 17α-propionate (I) involves hydrolyzing an ortho-ester derivative (II) in the presence of at least one acid selected from formic acid, ascorbic acid, benzoic acid, aluminium trichloride (AlCl3) and its mixtures to obtain cortexolone 17α-propionate (I). USE - Process for preparing cortexolone 17α-propionate (I), for treating acne vulgaris in patients. No biological data given. ADVANTAGE - The cortexolone 17α-propionate (I) has high purity more than 95%,less content of impurities. The process is easy, robust and reproducible on a commercial scale, and does not require pH control. DETAILED DESCRIPTION - Preparing cortexolone 17α-propionate of formula (I) involves hydrolyzing an ortho-ester derivative of formula (II) in the presence of at least one acid selected from formic acid, ascorbic acid, benzoic acid, aluminium trichloride (AlCl3) and its mixtures to obtain cortexolone 17α-propionate of formula (I). R1=hydrogen or a methyl. An INDEPENDENT CLAIM is included for a process for the preparation of crystalline Form III of cortexolone 17α-propionate (I) which involves (a) ortho-esterification of cortexolone of formula (III) in the presence of a reagent selected from triethyl orthopropionate and trimethyl orthopropionate, to provide the ortho-ester derivative (II); (b) hydrolyzing the ortho-ester derivative (II) in the presence of at least one acid selected from formic acid, ascorbic acid, benzoic acid, aluminium trichloride (AlCl3) to obtain cortexolone 17α-propionate (I); and (c) crystallizing cortexolone 17α-propionate (I) which comprises (i) providing a solution of cortexolone 17α-propionate in ethanol; (ii) combining the solution of cortexolone 17α-propionate with n-hexane to obtain a mixture; (iii) maintaining the mixture obtained at 0-5 ℃ (± 2 ℃), and stirring the mixture for 25-35 minutes; and (iv) isolating crystalline form III of cortexolone 17α-propionate.
IPC 分类号	A61K-031/573 ; A61P-015/16 ; A61P-017/00 ; A61P-005/28 ; C07J-005/00 ; C12P-033/00
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/20427
专题	中国科学院新疆生态与地理研究所
作者单位	PULSE PHARM PVT LTD (PULS-Non-standard)
推荐引用方式 GB/T 7714	KATRAGADDA V R,KUNDETI P,RAVURI S,et al. Preparing cortexolone 17 alpha-propionate, for treating acne vulgaris in patients involves hydrolyzing an ortho-ester in the presence of at least one acid selected from formic acid, ascorbic acid, benzoic acid, aluminium trichloride and its mixtures to obtain cortexolone 17alpha-propionate. IN202341061366-A[P]. 2023.

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