Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl) amides: A late-stage diversification approach to potent 5HT 1B antagonists

CL Horchler, JP McCauley, JE Hall, DH Snyder…

Index: Horchler, Carey L.; McCauley Jr., John P.; Hall, James E.; Snyder, Dean H.; Craig Moore; Hudzik, Thomas J.; Chapdelaine, Marc J. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 2 p. 939 - 950

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Citation Number: 25

Abstract

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 ...