Development of an Acyl Sulfonamide Anti-Proliferative Agent, LY573636· Na†

MH Yates, NJ Kallman, CP Ley…

文献索引：Yates, Matthew H.; Kallman, Neil J.; Ley, Christopher P.; Wei, Jeffrey N. Organic Process Research and Development, 2009 , vol. 13, # 2 p. 255 - 262

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被引用次数: 14

摘要

The synthesis of 5-bromo-thiophene-2-sulfonic acid 2, 4-dichlorobenzoylamide sodium salt on multikilogram scale is described. The initial clinical supplies were made using carbonyl diimidazole to converge the two fragments. A more efficient acid chloride process has been developed, which also provides better control of impurities and color throughout the synthesis.