醋酸甲地孕酮中相关杂质的表征

Characterization of related impurities in megestrol acetate.

作者信息

Guo Fujiang, Feng Huijin, Wang Youfu, Zhang Chune, Li Yuanchao

机构信息

Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China.

出版信息

J Pharm Biomed Anal. 2006 Jun 16;41(4):1418-22. doi: 10.1016/j.jpba.2006.02.048. Epub 2006 Apr 17.

DOI:10.1016/j.jpba.2006.02.048

PMID:16616448

Abstract

Three new compounds, 17alpha-acetoxy-2,6-dimethylpregna-1,4,6-triene-3,20-dione (1), 17alpha-acetoxy-2alpha,6-dimethylpregna-4,6-diene-3,20-dione (2), 17alpha-acetoxy-6alpha-methoxylmethylpregna-4-ene-3,20-dione (3), together with five known ones, 17alpha-acetoxy-6beta-hydroxyl-6alpha-methylpregna-4-ene-3,20-dione (4), 17alpha-acetoxy-6alpha-hydroxyl-6beta-methylpregna-4-ene-3,20-dione (5), 17alpha-acetoxy-pregna-4-ene-3,6,20-trione (6), 17alpha-acetoxy-pregna-4-ene-3,20-dione (7) and 17alpha-acetoxy-6-methylene-pregna-4-ene-3,20-dione (8), were isolated and identified from the residual mother liquor of megestrol acetate. Their structures were established by spectroscopic methods. These compounds seem to be minor impurities in production of the drug megestrol acetate.

摘要

从醋酸甲地孕酮的残留母液中分离并鉴定出三种新化合物，17α-乙酰氧基-2,6-二甲基孕甾-1,4,6-三烯-3,20-二酮（1）、17α-乙酰氧基-2α,6-二甲基孕甾-4,6-二烯-3,20-二酮（2）、17α-乙酰氧基-6α-甲氧基甲基孕甾-4-烯-3,20-二酮（3），以及五种已知化合物，17α-乙酰氧基-6β-羟基-6α-甲基孕甾-4-烯-3,20-二酮（4）、17α-乙酰氧基-6α-羟基-6β-甲基孕甾-4-烯-3,20-二酮（5）、17α-乙酰氧基-孕甾-4-烯-3,6,20-三酮（6）、17α-乙酰氧基-孕甾-4-烯-3,20-二酮（7）和17α-乙酰氧基-6-亚甲基-孕甾-4-烯-3,20-二酮（8）。它们的结构通过光谱方法确定。这些化合物似乎是醋酸甲地孕酮生产过程中的微量杂质。