A New Addition Compound of Desloratadine with Carbon Dioxide
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- 作者：Tibor Mezei ; Balá ; zs Volk ; Imre Kirá ; ly ; Gyula Simig
- 刊名：Organic Process Research & Development
- 出版年：2008
- 出版时间：September 19, 2008
- 年：2008
- 卷：12
- 期：5
- 页码：855-859
- 全文大小：130K
- 年卷期：v.12,no.5(September 19, 2008)
- ISSN：1520-586X
文摘
The addition compound of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (descarboethoxyloratadine, desloratadine) with CO2, in molar ratio 2:1, is described. This unique form of desloratadine drug substance can be prepared in exceedingly high purity by a simple process from crude desloratadine. The addition compound is a useful intermediate in the manufacturing process of desloratadine Form I polymorph. An improved, environmental friendly manufacturing process for the synthesis of desloratadine starting from loratadine is also disclosed here.