A practical and scaleable synthesis of A-224817.0, a novel nonsteroidal ligand for the glucocorticoid receptor

…, T Grieme, P Raje, P Sharma, HE Morton…

Index: Ku, Yi-Yin; Grieme, Tim; Raje, Prasad; Sharma, Padam; Morton, Howard E.; Rozema, Mike; King, Steve A. Journal of Organic Chemistry, 2003 , vol. 68, # 8 p. 3238 - 3240

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Citation Number: 28

Abstract

A practical and scaleable synthesis of a novel nonsteroidal ligand for the glucocorticoid receptor A-224817.0 1A is described. The synthesis proceeds in seven steps starting from 1, 3-dimethoxybenzene. The biaryl intermediate 5 was prepared by an optimized high-yielding and high-throughput Negishi protocol. The quinoline core 8 was constructed by using a modified Skraup reaction. The final product was obtained by a direct allylation reaction of ...