✦ LIBER ✦
Preparation of 14C-labeled 8,9-didehydro-6,8-dimethyl-2-methylthioergoline mesylate, a dopamine antagonist potentially useful in the treatment of schizophrenia
✍ Scribed by William J. Wheeler
- Publisher
- John Wiley and Sons
- Year
- 1988
- Tongue
- French
- Weight
- 381 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
We have prepared 14C-labeled 8,9--6,8-dimethy1-2-methylthioergoline mesylate (LY 170542), a U e antagonist potentially useful as an anti-psychotic. The 14C-label was introduced via a novel application of the Wittig reaction on 1-(4'-toluene-sulfonyl) -8,9-didehydr&6-meth 1 lysergene by lithiudammonia at -33OC. The 17-[14Cl-agroclavine thus prepared was converted into 17-[ 14C]-LY 170542 by reaction with methanesulfenyl chloridelmethanesulfonic acid ergolin-8-one and subsequent reduction of 1-(4'-toluenesulfonyl)-17-[ ? -