文献类型：期刊文章

作　　者：王莅[1] 祝翠红[2] 张香文[1] 米镇涛[1]

机构地区：[1]天津大学化工学院,天津300072 [2]天津药业有限公司技术开发部

出　　处：《应用化学》

基　　金：天津药业有限公司博士后科研基金资助 ( 19990 2 )

年　　份：2002

卷　　号：19

期　　号：12

起止页码：1189-1191

语　　种：中文

收录情况：AJ、BDHX、BDHX2000、CAS、CSCD、CSCD2011_2012、JST、RSC、ZGKJHX、核心刊

摘　　要：Hydroxy-16α,17α,21-trimethyl-5-en-20-one was synthesized from 3α-acetoxypregna-5,16-dien-20-one and characterized by elemental analysis, 1H NMR, MS and IR. 16α,17α-Dimethyl steroid was formed by treatment of 3β-acetoxypregna-5,16-dien-20-one with methylmagnesium bromide, followed by reaction of the resulting 17(20)-enolate with methyl iodide. The main by- products were 3β-hydroxy-16α,17α-dimethyl-5-en-20-one. LHDMS([(CH 3) 3Si] 2NLi) and LDA([(CH 3) 2CH] 2NLi) were chosen as proper reagents for 21-position alkylation. The almost quantitative conversion of 16α,17α-dimethyl corticosteroid was achieved and the highest yield of the 16α,17α,21-trimethyl corticosteroid was 78%. The optimum reaction temperature was -20 ℃ for 16α,17α- dialkylation and was -50 ℃ for 21- position alkylation.

关 键 词：3β-羟基-16α,17α,21-三甲基孕甾-5-烯-20-酮  合成  皮质激素 甲基化 共轭加成 瑞美松龙  眼科甾体抗炎药物  

分 类 号：TQ463.34[化工与制药类] R98]