Synthese d'un diuretique marque au carbone 14: Acide dichloro‐2,3 [thenoyl‐2 (14C = 0)]‐4 phenoxy acetique (D.C.I. acide tiénilique)
- 1 July 1976
- journal article
- research article
- Published by Wiley in Journal of Labelled Compounds and Radiopharmaceuticals
- Vol. 12 (3) , 437-441
- https://doi.org/10.1002/jlcr.2580120313
Abstract
2‐Thenoic acid (14C = 0) 1 is prepared in 75 % radioactive yield by carbonation with 14CO2 of 2‐thienyL‐magnesium bromide. Boiling of 1 with oxalyl chloride gives rise to 2‐thenoylchloride (14CO) which is not isolated and is condensed with 2,3 dichLoroanisoLe under FrieLdeL‐Grafts conditions. Ketone 3 is demeth Lated with AlCl3 in benzene to give rise to 4‐ 2‐thenoyl (14C = O)‐2,3‐dichloro phenol 4. The sodium derivative of 4 is condensed in D.M.F. with sodium chloracetate to Lead to the title compound with an overall yield of 16 % based on 14CO2 – TieniLic acid‐14c, specific activity: 50 mCi/mMole, has been found to be sensitive to self‐irra‐diation decomposition in the dry state at ‐ 25%° C. Radiation decomposition is minimized at 24 mCi/mMole in methanol solution.This publication has 0 references indexed in Scilit: