Radiosynthesis of 6-([18F]fluoroacetamido)-1-hexanoic-anilide ([18F]FAHA) for PET imaging of histone deacetylase (HDAC)
Radiosynthesis of 6-([18F]fluoroacetamido)-1-hexanoic-anilide ([18F]FAHA) for PET imaging of histone deacetylase (HDAC)
复制标题
6-([18F]氟乙酰胺)-1-己酰苯胺 ([18F]FAHA) 的放射合成用于组蛋白脱乙酰酶 (HDAC) 的 PET 成像
DOI：
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发表时间：
2006
期刊：
影响因子：
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通讯作者：
M. Alauddin
中科院分区：
文献类型：
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作者：
U. Mukhopadhyay;W. Tong;J. Gelovani;M. Alauddin
报道了组蛋白去乙酰化酶（HDAC）底物6-（[18 F]氟乙酰氨基）-1-己酰苯胺（[18 F]FAHA，[18 F]-3）的放射合成。对于前体合成，通过6-氨基己酸与亚硫酰氯在二氯乙烷中反应，随后加入苯胺来制备化合物1（6-氨基-1-己酰苯胺）。化合物1与溴乙酸酐在四氢呋喃（THF）中在三乙胺的存在下反应以产生前体化合物6-（溴乙酰氨基）-1-己酰苯胺2。使用氟化四丁基铵在各种溶剂中在80°C下进行氟化反应以制备未标记的参比化合物3。使用n-Bu 4 N18 F或K18 F/kryptofix进行放射性氟化，并通过高效液相色谱法（HPLC）纯化粗产物。放射化学产额为9-13%衰变校正（d.c.）使用K18 F/kryptofix，平均值为11%，合成结束时比活度>2 GBq/µmol。合成时间为从轰击结束（EOB）起67-75分钟。版权所有© 2006约翰威利父子有限公司。
Radiosynthesis of a novel substrate for histone deacetylase (HDAC), 6-([18F]fluoroacetamido)-1-hexanoicanilide ([18F]FAHA, [18F]-3) is reported. For precursor synthesis, compound 1 (6-amino-1-hexanoicanilide) was prepared by the reaction of 6-amino hexanoic acid with thionyl chloride in dichloroethane followed by addition of aniline. Compound 1 was reacted with bromoacetic anhydride in tetrahydrofuran (THF) in the presence of triethylamine to produce the precursor compound 6-(bromoacetamido)-1-hexanoicanilide 2. Fluorination reactions were performed using tetrabutylammonium fluoride in various solvents at 80°C to prepare the unlabeled reference compound 3. Radiofluorinations were performed using either n-Bu4N18F or K18F/kryptofix, and the crude product was purified by high performance liquid chromatography (HPLC). The radiochemical yields were 9–13% decay corrected (d.c.) with an average of 11% using K18F/kryptofix, and specific activity >2 GBq/µmol at the end of synthesis. The synthesis time was 67–75 min from the end of bombardment (EOB). Copyright © 2006 John Wiley & Sons, Ltd.
烷基取代的聚氨基异羟肟酸：一类新型的靶向组蛋白脱乙酰酶抑制剂。
影响因子：
7.3
作者：
Varghese,Sheeba;Gupta,Deepak;Baran,Tiffany;Jiemjit,Anchalee;Gore,StevenD;CaseroJr,RobertA;Woster,PatrickM
通讯作者：
Woster,PatrickM