Me[18F]FBWAY

Chemical Name: 4-(18Fluoro)-3-methyl-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-(2-pyridinyl)benzamide
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线: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.