Synthesis of 2, 6-difluoro-N-(3-[11 C] methoxy-1H-pyrazolo [3, 4-b] pyridine-5-yl)-3-(propylsulfonamidio) benzamide as a new potential PET agent for imaging of B-Raf …

M Wang, M Gao, KD Miller, QH Zheng

Index: Wang, Min; Gao, Mingzhang; Miller, Kathy D.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2013 ,  vol. 23,  # 4  p. 1017 - 1021

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Citation Number: 9

Abstract

The authentic standard 2, 6-difluoro-N-(3-methoxy-1H-pyrazolo [3, 4-b] pyridine-5-yl)-3- (propylsulfonamidio) benzamide was synthesized from 2, 6-difluorobenzoic acid and 3- amino-5-hydroxypyrazole in 9 steps with 1% overall chemical yield. Direct desmethylation of the reference standard with TMSCl/NaI gave the precursor 2, 6-difluoro-N-(3-hydroxy-1H- pyrazolo [3, 4-b] pyridine-5-yl)-3-(propylsulfonamidio) benzamide for radiolabeling in 70% ...