Abstract
[ 3 H]-Cyclosporin A labeled at the first amino acid ([ω- 3 H-MeBmt 1 ]CS) has been prepared by tritium gas hydrogenolysis of [O-acetyl-ω-bromo-MeBmt 1 ]CS followed by deprotection with methanolic sodium methoxide. The requisite bromo intermediate was prepared by bromination of [O-acetyl-MeBmt 1 ]CS with N-bromosuccinimide. After synthesis and purification, 2.45 mg of [ω 3 H-MeBmt 1 ]CS with a total activity of 327 MBq were produced with a radiochemical purity >97 %, and specific activity of 160 GBq/mmol (4.3 Ci/mmol).
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