๐”– Bobbio Scriptorium
โœฆ   LIBER   โœฆ

Synthesis of 14C-labelled etintidine hydrochloride

โœ Scribed by Stephen M. Stefanick; Charles F. Kasulanis; Seymour D. Levine; Arthur C. Fabian

Publisher
John Wiley and Sons
Year
1985
Tongue
French
Weight
279 KB
Volume
22
Category
Article
ISSN
0022-2135

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โœฆ Synopsis

Two 14C preparations o f t h e Hz-antagonist e t i n t i d i n e hydrochloride a r e reported.

I n one, t h e l a b e l I s introduced by r e a c t i n g [1-I4C] propargylamine w i t h t h e a p p r o p r i a t e i s o t h i ourea, f o l l o w e d by h y d r o c h l o r i d e formation. This a f f o r d e d a m a t e r l a l o f 95% radlochemlcal p u r i t y whose s p e c i f i c a c t i v l t y was 1.5 mCi/mnol. To o b t a i n m a t e r i a l l a b e l l e d i n an a l t e r n a t e p o s i t i o n . u n i f o r m l y l a b e l l e d 14C-cysteamine hydrochloride was reacted w i t h 4-methyl-5-hydroxymethyl Imldazole hydrochloride t o produce 4methyl-5-[(2-aminoethyl)thiomethyl]lmidazole.

This was converted i n t h r e e a d d i t i o n a l steps t o e t i n t i d i n e h y d r o c h l o r l d e y i e l d i n g m a t e r i a l o f 96% radlochemlcal p u r i t y and s p e c i f i c a c t i v i t y o f 9.0 mCl/mnol.

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