A novel no‐carrier‐added submicromolar scale radiosynthesis of [S‐methyl‐14C]‐florfenicol |
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Authors: | G Srinivas G Prabhakar V K P Unny K Sudhakar K Mukkanti B M Choudary |
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Institution: | 1. Radiolabelling Department, , Hyderabad, 500037 Andhra Pradesh, India;2. Centre for Pharmaceutical Sciences I S T, Jawaharlal Nehru Technological University, , Hyderabad, 500085 Andhra Pradesh, India |
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Abstract: | In this paper is reported a novel reaction scheme for the no‐carrier‐added submicromolar scale radiosynthesis of S‐methyl‐14C]‐florfenicol that has been newly designed, developed and employed by us successfully. The 14C]‐product was obtained in an overall radiochemical yield of 30% based on 14C]‐methyl iodide taken for the reaction with a radiochemical purity of more than 96%. The specific activity of the product was ~50 mCi (1.85 GBq)/mmol. Chlorosulfonation of compound I was followed by sodium salt formation in situ and it was succeeded by the introduction of 14C]‐methyl group by coupling with 14C]‐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‐14C]‐florfenicol. |
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Keywords: | radiosynthesis of [S‐methyl‐14C]‐florfenicol radioisotopically labeled florfenicol S‐methylation [14C]‐methyl iodide |
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