## Abstract The synthesis of Asaley labelled with ^14^C in the mustard (Asaleyβmustβ^14^C) or the leucine (Asaleyβleuβ^14^C) moiety is described. In the former, ethyl paminoβN^Ξ±^βacetylβDLβphenylalanylβLβleucinate was reacted with ethylene oxide(U)β^14^C to give the bis(hydroxyethyl)amino analogue,
Syntheses of 14C-labelled prizidilol dihydrochloride
β Scribed by D Saunders; B H Warrington
- Publisher
- John Wiley and Sons
- Year
- 1985
- Tongue
- French
- Weight
- 396 KB
- Volume
- 22
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
β¦ Synopsis
Two syntheses o f r a d i o l a b e l l e d p r i z i d l l o l d i h y d r o c h l o r l d e (DL)3-[2-(3-t-butylamino -2-hydroxypropoxy)phenyl]-6-hydrazinop y r i d a z l n e d i h y d r o c h l o r i d e ) a r e described. 1. A t e n stage synthesis (Scheme 1) which gave 14 [3,6y i e l d o f 0.91%. C2] p r i z l d l l o l d l h y d r o c h l o r l d e (0) I n an o v e r a l l 2. A l a t e r , a l t e r n a t i v e procedure (scheme 2) leading t o 14 [4,5-C2] p r i z i d i l o l d i h y d r o c h l o r i d e (B) w i t h an o v e r a l l radiochemical y i e l d o f 8%. 14 Keywords: P r i z i d i l o l d i h y d r o c h l o r i d e , [1,4acid, [2,3-C2] s u c c i n i c anhydrtde, p r e p a r a t i v e l a y e r chromatography, reverse i s o t o p e d i l u t i o n , 14C-labelled.
π SIMILAR VOLUMES
14C-Labelled 6-hydroxy-5,7-dimethyl-2-(methylamino)-4-(3-pyridylmethyl)benzothiazole dihydrochloride (14C-E3040 dihydrochloride), required for a study of the phrmacokinetic profile of E3040, a novel dual inhibitor of 5-lipoxygenase and thromboxane A2 synthetase, was synthesized in one step using [2-
Convenient methods for the selective hydrolysis of the thioester groups of dithiopyr to the corresponding carboxylic acid are described. 2-@ifluoromethyl)-4-(2-methylpropyl)-5-[ (methylthio)carbnyl] -6-(trifluoromethyl)-3-pyridine-4-~~C-carboxylic acid (2) was obtained by simple potassium hydroxide
The hlstamlne H1 agonlst, 2-[2-14C]-(2-amlnoethyl)-thlazole dlhydrochlorlde has been l a b e l l e d w t t h carbon-14 I n the 2 p o s l t l o n of the t h l a z o l e s t a r t l n g from potasslum [14C] cyanlde. The o v e r a l l radlochemlcal y i e l d f o r the synthesls was 17% a t a s p e c i
## 4-[4-(4-Chlorophen y l ) -4-hydroxypiperidinol -4 ' -f l u o r o b u t y r op h e n o n e ( h a l o p e r i d o l ) ( I ) and 4'-fluoro-4-[4-hydroxy-4-(3-trif 1 u o r o m e t h y l p h e n y l ) p i p e r i d i n o l b u t y r o p h e n o n e ( t r i f 1 u p e r i d o f ) (11) , n e u r o l e p t
14C-Labelled satigrel, or 4-cyano-5-(4'-methoxy tring-U-14CI phenyl)-5-(4"methoxyphenyl)-4-pentenoic acid was synthesized for drug metabolism and pharmacokinetic studies using 4,4'-diniethoxy [ring-U-W ] benzophenone as the starting material. The radiochemical yield was 10.0%. The specific radioacti