Carey L. Horchler, John P. McCauley Jr., James E. Hall, Dean H. Snyder, W. Craig Moore, Thomas J. Hudzik, and Marc J. Chapdelaine. AstraZeneca Pharmaceuticals LP, Wilmington, DE
Multiparallel amenable syntheses of 6-methoxy-8-amino-4-oxo-1,4-dihydroquinoline-2-carboxylic acid-(4-morpholin-4-yl-phenyl)amides (I) and 4-amino-6-methoxy-8-(4-methyl-piperazin-1-yl)-quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides (II) which facilitate late-stage diversification at the 8-position of (I) and at the 4- and 8-positions of (II) are described. The resulting novel series were determined to contain potent 5HT1B antagonists. Preliminary SAR data is presented.
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