Development of a Scaleable Synthesis of a Partial Nicotinic Acid Receptor Agonist
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- 作者：Robert D. Wilson ; Ed Cleator ; Michael S. Ashwood ; Matthew M. Bio ; Karel M. J. Brands ; Antony J. Davies ; Ulf-H. Dolling ; Khateeta M. Emerson ; Andrew D. Gibb ; David Hands ; Arlene E. McKeown ; Steven F. O
- 刊名：Organic Process Research & Development
- 出版年：2009
- 出版时间：May 15, 2009
- 年：2009
- 卷：13
- 期：3
- 页码：543-547
- 全文大小：157K
- 年卷期：v.13,no.3(May 15, 2009)
- ISSN：1520-586X
文摘
A practical and efficient synthesis of 1,4,5,6-tetrahydro-3-(1H-tetrazol-5-yl)cyclopenta[c]pyrazole, 1, is described. A new one-pot process has been developed, starting from the commercially available 1H-tetrazole-5-carboxylic acid-ethyl ester sodium salt which is reacted in a pseudo-Claisen condensation reaction with cyclopentanone, followed by the addition of hydrazine.