کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2029275 | 1070533 | 2013 | 6 صفحه PDF | دانلود رایگان |
Spironolactone is a renal competitive aldosterone antagonist. One of its most important metabolite is the 7α-methylthio spironolactone: thus it is very important to have an efficient and safe access to this compound, for pharmacokinetic studies. In this context, we synthesized this metabolite by thioalkylation of 7α-thio spironolactone using Hünig’s base with a very good yield. We also used our procedure to prepare, with an easy work-up and high yields, 7α-thioether and thioester derivatives of spironolactone, that could be useful for further Structure–Activity Relationships studies.
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► Efficient synthesis of the 7α-methylthioether metabolite of spironolactone.
► Green approach of 7α-thioether and thioester spironolactone derivatives.
► Small library of C19 steroids, having a spirannic γ-lactone at the C-17.
Journal: Steroids - Volume 78, Issue 1, January 2013, Pages 102–107