A novel no-carrier-added submicromolar scale radiosynthesis of [S-methyl-C-14]-florfenicol

作者：Srinivas G; Prabhakar G; Unny V K P^*; Sudhakar K; Mukkanti K; Choudary B M

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2013, 56(8): 382-384.

DOI：10.1002/jlcr.3053

• radiosynthesis of [S-methyl-C-14]-florfenicol
• radioisotopically labeled florfenicol
• S-methylation
• [C-14]-methyl iodide

In this paper is reported a novel reaction scheme for the no-carrier-added submicromolar scale radiosynthesis of [S-methyl-C-14]-florfenicol that has been newly designed, developed and employed by us successfully. C-14]-product was obtained in an overall radiochemical yield of 30% based on [C-14]-methyl iodide taken for the reaction with a radiochemical purity of more than 96%. in situ and it was succeeded by the introduction of [C-14]-methyl group by coupling with [C-14]-CH3I. Subsequently, the oxazolidin-2-one protecting group was opened up by a reaction with sulfuric acid in dioxane and later, the amino group was dichloroacetylated with methyl-2,2-dichloroacetate in triethylamine to obtain [S-methyl-C-14]-florfenicol.

• 出版日期2013-6-30