干旱区生态环境知识资源中心(Arid): Automated Optimized Synthesis of [18F]FLT Using Non-Basic Phase-Transfer Catalyst with Reduced Precursor Amount

Arid

DOI	10.3390/molecules27238323
	Automated Optimized Synthesis of [18F]FLT Using Non-Basic Phase-Transfer Catalyst with Reduced Precursor Amount
	Fedorova, Olga S.; Orlovskaya, Viktoriya V.; Krasikova, Raisa N.
通讯作者	Krasikova, RN
来源期刊	MOLECULES
EISSN	1420-3049
出版年	2022
卷号	27 期号:23
英文摘要	3 & PRIME;-deoxy-3 & PRIME;-[F-18]fluorothymidine ([F-18]FLT) is a positron emission tomography (PET) tracer useful for tumor proliferation assessment for a number of cancers, particularly in the cases of brain, lung, and breast tumors. At present [F-18], FLT is commonly prepared by means of the nucleophilic radiofluorination of 3-N-Boc-5'-O-DMT-3'-O-nosyl thymidine precursor in the presence of a phase-transfer catalyst, followed by an acidic hydrolysis. To achieve high radiochemical yield, relatively large amounts of precursor (20-40 mg) are commonly used, leading to difficulties during purification steps, especially if a solid-phase extraction (SPE) approach is attempted. The present study describes an efficient method for [F-18]FLT synthesis, employing tetrabutyl ammonium tosylate as a non-basic phase-transfer catalyst, with a greatly reduced amount of precursor employed. With a reduction of the precursor amount contributing to lower amounts of synthesis by-products in the reaction mixture, an SPE purification procedure using only two commercially available cartridges-OASIS HLB 6cc and Sep-Pak Alumina N Plus Light-has been developed for use on the GE TRACERlab FX N Pro synthesis module. [F-18]FLT was obtained in radiochemical yield of 16 +/- 2% (decay-corrected) and radiochemical purity > 99% with synthesis time not exceeding 55 min. The product was formulated in 16 mL of normal saline with 5% ethanol (v/v). The amounts of chemical impurities and residual solvents were within the limits established by European Pharmacopoeia. The procedure described compares favorably with previously reported methods due to simplified automation, cheaper and more accessible consumables, and a significant reduction in the consumption of an expensive precursor.
英文关键词	fluorine-18 radiofluorination automated synthesis 3 '-deoxy-3 '-[F-18]fluorothymidine [F-18]FLT solid phase extraction
类型	Article
语种	英语
开放获取类型	Green Published, gold
收录类别	SCI-E
WOS记录号	WOS:000898020600001
WOS关键词	F-18-FLUOROTHYMIDINE PET ; PROLIFERATION ; CANCER ; CHEMORADIOTHERAPY ; PURIFICATION ; FLUORINATION
WOS类目	Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
资源类型	期刊论文
条目标识符	http://119.78.100.177/qdio/handle/2XILL650/393821
推荐引用方式 GB/T 7714	Fedorova, Olga S.,Orlovskaya, Viktoriya V.,Krasikova, Raisa N.. Automated Optimized Synthesis of [18F]FLT Using Non-Basic Phase-Transfer Catalyst with Reduced Precursor Amount[J],2022,27(23).
APA	Fedorova, Olga S.,Orlovskaya, Viktoriya V.,&Krasikova, Raisa N..(2022).Automated Optimized Synthesis of [18F]FLT Using Non-Basic Phase-Transfer Catalyst with Reduced Precursor Amount.MOLECULES,27(23).
MLA	Fedorova, Olga S.,et al."Automated Optimized Synthesis of [18F]FLT Using Non-Basic Phase-Transfer Catalyst with Reduced Precursor Amount".MOLECULES 27.23(2022).