Development of an Efficient Synthesis for a Nipecotate-Containing Immunopotentiator

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• 作者：Eric D. Moher ; Allie E. Tripp ; Lawrence C. Creemer ; and Jeffrey T. Vicenzi
• 刊名：Organic Process Research & Development
• 出版年：2004
• 出版时间：July 2004
• 年：2004
• 卷：8
• 期：4
• 页码：593 - 596
• 全文大小：54K
• 年卷期：v.8,no.4(July 2004)
• ISSN：1520-586X

文摘

The preparation of Elanco Animal Health immunopotentiator(S)-ethyl-1-(2-thiopheneacetyl)-3-piperidinecarboxylate (1) isdescribed. The synthesis includes a new resolution of racemicethyl nipecotate with dibenzoyl-L-tartaric acid. The resolvedsalt is found to couple directly with commercially available2-thiopheneacetyl chloride under environmentally friendlySchotten-Baumann conditions to afford the amide in high yield.The final product is an oil which is purified by wiped filmevaporative distillation.