Synthesis of Biologically Active Heterocyclic Compounds Labelled with Positron Emitting Radionuclides for Diagnoses of Diseases of Brain and Heart and Cancer

建立了一种以[^ F]氟化物为原料合成[氟乙酰-^<18>F]氟褪黑素（N^<omega>- [^<18>F] Fluoroacetyl-5-methoxytryptamine）<18>的有效方法。[^<18>F]氟化物是使用东北大学回旋加速器，从循环的20%浓缩[^ O]水靶中通过^<18>O（p，n）^<18>F核反应产生<18>的。由此形成的^<18>F核素转化为氟化钾[^<18>F]。由<18>溴代乙酸乙酯与对甲苯磺酸银反应生成对甲苯磺酰氧基乙酸乙酯，再与[~（14）F]氟反应生成[~（14）<18>F]氟乙酸乙酯，然后用碱水解，在二环己基碳二亚胺存在下与5-甲氧基色胺缩合，得到目标放射性同位素，放化产率为26.7%。其纯度&gt; 98%，比活度为540 mCi/mumol，合成所需总时间约90 min，在类似条件下合成了N^<omega>- [^<18>F]氟乙酰5-羟色胺，放化产率为22.6%。该激素的纯度&gt;98%，比活性为600 mCi/mumol。

An efficient synthesis of [fluoroacetyl-^<18>F] fluoromelatonin (N^<omega>- [^<18>F] Fluoroacety1-5-methoxytryptamine) starting from [^<18>F]fluoride has been established. [^<18>F] Fluoride was produced by the ^<18>O (p, n)^<18>F nuclear reaction from a circulating 20%-enriched [^<18>O] water target using the Tohoku University Cyclotron. The ^<18>F nuclide thereby formed was converted to potassium [^<18>F] fluoride. The reaction of[^<18>F]fluoride with ethyl p-toluenesulfonyloxyacetate derived from ethyl bromoacetate with silver p-toluenesulfonate afforded ethyl [^<18>F] fluoroacetate, which was then hydrolyzed with alkali and condensed with 5-methoxytryptamine in the presence of dicyclohexylcarbodiimide to give the desired radioactive isotope in a 26.7% radiochemical yield. The purity, specific activity and the total time required for its synthesis are>98%, 540 mCi/mumol and ca.90 min, respectively.N^<omega>- [^<18>F] Fluoroacetylserotonin was synthesized under similar conditions in 22.6% radiochemical yield. The purity and specific activity of the hormone are>98% and 600 mCi/mumol, respectively.