Syntheses of di-tritiated 9(O)-methano-Δ6(9α)-prostaglandin I1 methyl esters
✍ Scribed by Kenji Manabe; Toshio Tanaka; Seizi Kurozumi; Yoshinori Kato
- Publisher
- John Wiley and Sons
- Year
- 1991
- Tongue
- French
- Weight
- 698 KB
- Volume
- 29
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
Two di‐tritiated isocarbacyclin [9(O)‐methano‐Δ^6^(9α)‐prostaglandin I~1~] methyl esters 5, 10 were synthesized from (Z)‐olefinic precursors 23, 31 at ω‐side chain by catalytic hydrogenation with tritium gas, respectively. These substances 5, 10 having high specific activities can be used for the pharmacokinetics and metabolism studies of 9(O)‐methano‐Δ^6(9α)^‐prostaglandin I~1~ methyl ester 2 and its (17S)‐17,20‐dimethyl derivatives 7.
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## A six-step synthesis of tritiated 6a, 9a-d~uoro-l6u-methyl-11~, 17u,21 -trihydroxypregna-l,4-diene-3,20-dione (5) and 6a,9a-di~?uoro-11 f3,16a,I 7aJI -tetrahydroxypregna-I ,4-diene-3,20-dione 16~7-aeetonide ( 7 ) from the appropriate A174?9(11)-3-keto intermediates is described. Isotope inco
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