DEIODOTRIFLUOROMETHYLATION OF ETHYL 3,3',5-TRIIODOTHYROACETATE - DIVERGENT DERIVATIZATION BASED ON THE COMBINATORIAL CONCEPT

Authors
SAGI K KAGECHIKA H FUKASAWA H HASHIMOTO Y SHUDO K
Citation
K. Sagi et al., DEIODOTRIFLUOROMETHYLATION OF ETHYL 3,3',5-TRIIODOTHYROACETATE - DIVERGENT DERIVATIZATION BASED ON THE COMBINATORIAL CONCEPT, Chemical and Pharmaceutical Bulletin, 44(6), 1996, pp. 1273-1275
Citations number
16
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
44
Issue
6
Year of publication
1996
Pages
1273 - 1275
Database
ISI
SICI code
0009-2363(1996)44:6<1273:DOE3-D>2.0.ZU;2-X
Abstract
A strategy for development of thyroid hormone analogs was examined bas ed on the combinatorial concept. The reaction of ethyl 3,3',5-triiodot hyroacetate (3b) with Cd/Br2CF2/CuBr followed by ester hydrolysis gave a mixture of more than ten products as detected by HPLC. The structur es of the products in the bioactive fractions showed that the replacem ent of iodides with trifluoromethyl groups is an effective approach fo r obtaining thyromimetics.