Betaniethasone 21 -acetate was catalytically reduced with tritium. The crude product was oxidized with 2,3-dichloro-5,6-dicyano-1,4benzoquinone ( D D Q ) to betamethasone-I,2,4JH 21-acetate. Hydrolysis gave bet~methasone-1,2,4-~H, which, when allowed to react with trimethylorthobenzoate, gave both b
Synthesis of betamethasone-l,2-3h2 17-benzoate
✍ Scribed by T. Kobari; S. Watanabe; S. Ikegami
- Publisher
- John Wiley and Sons
- Year
- 1975
- Tongue
- French
- Weight
- 241 KB
- Volume
- 11
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
A new convenient method for the preparation of the title compound is described. The method consists of selective tritiation of betamethasone 17‐benzoate (9α‐fluoro‐11β,17,21‐trihydroxy‐16β‐methyl‐1,4‐pregnadiene‐3,20‐dione 17‐benzoate) (1) with the use of tris(triphenylphosphine)rhodium chloride as catalyst, followed by dehydrogenation with 2,3‐dichloro‐5,6‐dicyano‐1,4‐benzoquinone (DDQ).
A favorable overall radiochemical yield is obtained.
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