Optimization of a convenient route to produce N-succinimidyl 4-radiodobenzoate for radioiodination of proteins
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Add time:08/23/2019 Source:sciencedirect.com
The preparation of N-succinimidyl-4-[131I]iodobenzoate (SIB) has been optimized using an alternative technique employing Cu(I)-assisted radioiododebromination that produces p-[131I]iodobenzoic acid. The reaction conditions were optimized and radiochemical purity of more than 90% was obtained when using 160°C, 60 min reaction time and a [CuCl]/[p-bromobenzoic acid] relation of about 10−2. After purification, the p-[131I]iodobenzoic acid reacted with TSTU to produce the SIB in a radiochemical yield greater than 98%. Protein conjugation using SIB resulted in a relatively low radiochemical yield. Biological distribution studies evidenced the in vivo stability of the labeled protein.
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