Abstract
A key intermediate, 4-aza-3-oxo-androstane-17β-carboxylic acid, for the preparation of some potent 5α-reductase inhibitors was synthesized in 5 steps from the known methyl 3-oxo-4-androstene-17β carboxylate. The construction of 4-aza-3-oxo-ring A of the steroid was achieved conveniently by a novel one-step simultaneous lactam formation and N-debenzylation of methyl 3-(2,4-dimethoxylbenzylamine)-5-oxo- A-nor-3,4-seco-androstane-17β -carboxylate with 4 equivalents of p-TsOH.
Original language | English |
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Pages (from-to) | 213-219 |
Number of pages | 7 |
Journal | Chinese Pharmaceutical Journal |
Volume | 55 |
Issue number | 3 |
Publication status | Published - 2003 Jun 1 |
All Science Journal Classification (ASJC) codes
- Pharmacology
- Pharmaceutical Science