Development of an Efficient Large-Scale Synthesis for a 4 H-imidazo [5, 1-c][1, 4] benzoxazine-3-carboxamide Derivative for Depression and Anxiety

…, AD Perboni, Z Cimarosti, P Westerduin…

文献索引：Giubellina, Nicola; Stabile, Paolo; Laval, Gilles; Perboni, Alcide D.; Cimarosti, Zadeo; Westerduin, Pieter; Cooke, Jason W. B. Organic Process Research and Development, 2010 , vol. 14, # 4 p. 859 - 867

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被引用次数: 8

摘要

The development and scale-up of an optimized synthesis for a novel drug candidate for depression and anxiety is presented. The updated synthesis represents a convergent and efficient four-stage approach to the API, overcoming high cost of goods (COG), general lack of convergence, and low yield of previous routes. A lower cost of goods resulted from using 3-nitrosalicylaldehyde as a starting material and introducing the expensive side chain (2- ...