Synthesis of [ω-3H-MeBmt1]-cyclosporin A

DOI: 10.1002/(SICI)1099-1344(199804)41:4<267::AID-JLCR79>3.0.CO;2-I

Source and publish data:

Journal of labelled compounds and radiopharmaceuticals p. 267 - 272 (1998)

Update date:2022-08-12

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Authors:

Cerny, Bohuslav

Jegorov, Alexandr

Polivkova, Jana

Sedmera, Petr

Havlicek, Vladimir

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Article abstract of DOI:10.1002/(SICI)1099-1344(199804)41:4<267::AID-JLCR79>3.0.CO;2-I

[³H]-Cyclosporin A labeled at the first amino acid ([ω-³H-MeBmt¹]CS) has been prepared by tritium gas hydrogenolysis of [O-acetyl-ω-bromo- MeBmt¹]CS followed by deprotection with methanolic sodium methoxide. The requisite bromo intermediate was prepared by bromination of [O-acetyl- MeBmt¹]CS with N-bromosuccinimide. After synthesis and purification, 2.45 m8 of [ω-³H-MeBmt¹]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).

Full text of DOI:10.1002/(SICI)1099-1344(199804)41:4<267::AID-JLCR79>3.0.CO;2-I

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