【药物名称】Me[18F]FBWAY
化学结构式(Chemical Structure):
参考文献No.537114
标题:Development of fluorine-18-labeled 5-HT1A antagonists
作者:Lang, L.; Jagoda, E.; Schmall, B.; Vuong, B.K.; Adams, H.R.; Nelson, D.L.; Carson, R.E.; Eckelman, W.C.
来源:J Med Chem 1999,42(9),1576
合成路线图解说明:

Condensation of 4-(dimethylamino)-3-methylbenzoic acid (I) with pentamethylbenzyl chloride (II) in the presence of Et3N afforded ester (III). The tertiary amino group of (III) was then methylated using methyl trifluoromethane-sulfonate to provide ammonium salt (IV). Subsequent displacement of the trimethylammonium salt of (IV) for a 18F-, followed by cleavage of the benzyl ester (V) with trifluoroacetic acid, provided the labeled intermediate 4-18fluoro-3-methylbenzoic acid (VI). Treatment of (VI) with dichloromethyl methyl ether gave the corresponding acid chloride (VII), which was finally coupled with amine (WAY 100634)(VIII) to produce the target amide.

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