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

已经建立了从[^<18>F]氟化物开始的[氟乙酰基-^<18>F]氟褪黑素（N^<omega>- [^<18>F]氟乙酰基-5-甲氧基色胺）的有效合成。[^<18>F]氟化物是由使用东北大学回旋加速器从循环20%富集的[^<18>O]水靶中产生的^<18>O (p, n)^<18>F核反应产生的。由此形成的^<18>F核素转化为[^<18>F]氟化钾。[^<18>F]氟与溴乙酸乙酯衍生的对甲苯磺酰氧乙酸乙酯和对甲苯磺酸银反应得到[^<18>F]氟乙酸乙酯，然后用碱水解，在双环己基碳二亚胺存在下与5-甲氧基色胺缩合，得到所需的放射性同位素，放射化学产率为26.7%。合成的纯度、比活性和总合成时间分别为0.98%、540 mCi/mumol和0.90 min。N^< ω >- [^<18>F]在类似条件下以22.6%的放射化学产率合成了氟乙酰血清素。该激素的纯度为60%，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.