The Chemical Development and Scale-Up of Sampatrilat1

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• 作者：Peter J. Dunn ; Michael L. Hughes ; Patricia M. Searle ; and Albert S. Wood
• 刊名：Organic Process Research & Development
• 出版年：2003
• 出版时间：May 2003
• 年：2003
• 卷：7
• 期：3
• 页码：244 - 253
• 全文大小：244K
• 年卷期：v.7,no.3(May 2003)
• ISSN：1520-586X

文摘

The discovery and scale-up of two routes to sampatrilat aredescribed. The first Chemical R and D route used a side productfrom another development project to accelerate drug supplyand expedite the early development programme. The second,more efficient Chemical R and D route had the potential forcommercialisation and used an environmentally friendly variantof the Baylis-Hillman reaction, and an asymmetric Michaeladdition as key steps. Full preparative details for the aminomethacrylate 4, a potentially useful chiral synthon, are givenfor the first time, along with full experimental details of theasymmetric Michael addition to make the chiral glutarate 5.Finally, a striking polymorph case history is described.