An Efficient and Scalable Synthesis of the Spirocyclic Glycine Transporter Inhibitor GSK2137305

…, JM Northall, AJ Roberts, AJ Whitehead

文献索引：Graham, Jonathan P.; Langlade, Nathalie; Northall, John M.; Roberts, Alastair J.; Whitehead, Andrew J. Organic Process Research and Development, 2011 , vol. 15, # 1 p. 44 - 48

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被引用次数: 9

摘要

An efficient and scalable synthesis of a glycine transporter inhibitor is presented. The key steps in the synthetic sequence are the formation of a spirocyclic imidazolidinone from an α- amino nitrile and a cyclic ketone and an arylation of 4-methyl imidazole under 'ligandless' Ullmann coupling conditions.