## Abstract The monoamine oxidase inhibitors pargyline and clorgyline have been synthesized by methylation of the appropriate secondary propargylamines, using [^14^C]dimethyl sulphate. This simple method should be generally applicable to other compounds of this class.
Synthesis of 3H- and 14C-labeled tracers for studies of functional monoamine oxidase activity
✍ Scribed by Christer Halldin; Peter Bjurling; Bengt Långström; Robert R. Macgregor; Joanna S. Fowler; Alfred P. Wolf
- Publisher
- John Wiley and Sons
- Year
- 1988
- Tongue
- French
- Weight
- 229 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
a m i n e a n d N-methylphenethyl amine as well as the 14C-labeling of c l o r g y l i n e a n d L -d e p r e n y l a r e d e s c r i b e d . L a b e l i n g was a c c o m p l i s h e d b y N -a l k y l a t l o n o f t h e f r e e b a s e o f t h e c o r r e s p o n d i n g d e s m e t h y l c o m p o u n d , u s i n g 3 H -m e t h y l I o d i d e , o r b y a r e d u c t i v e a l k y l a t i o n u s i n g p r o d u c t s were p u r i f i e d b y s e m i p r e p a r a t i v e HPLC. T h e t o t a l 4 C -f o r m a l d e h y d e . T h e c r u d e r a d i o c h e m i c a l y i e l d was 3 1 -6 5 % b a s e d o n ' H -m e t h y l I o d i d e a n d 6 0 % b a s e d o n 1 4 C -f o r m a l d e h y d e . T h e r a d i o c h e m i c a l p u r i t y was g r e a t e r t h a n 99 %. Key W o r d s : 3 H -l a b e l i n g , 1 4 C -l a b e l i n g , c l o r g y l i n e , L -d e p r e n y l , Y,N-dimethylphenethyl amine, x-methyluhenethyl amine * P r e s e n t a d d r e s s : K a r o l i n s k a P h a r m a c y , Box 6 0 0 2 4 , S -1 0 4 0 1 ** S t o c k h o l m , S w e d e n , To whom c o r r e s p o n d e n c e s h o u l d b e a d d r e s s e d 0362-4803/88/050~~$05 .OO @ 1988 by John Wiley & Sons, Ltd.
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## Abstract N‐[3‐(2,4‐dichlorophenoxy)propyl]‐N‐methyl‐2‐propynylamine‐1‐^14^C (^14^C‐clorgyline, **1a**) and L‐N, α‐dimethyl‐N‐2‐propynyl‐1‐^14^C‐phenethylamine (^14^C‐L deprenyl, **1b**) were synthesized by the Mannich reaction of 2‐methyl‐3‐butyn‐2‐ol, ^14^C‐formaldehyde, and secondary amines 3‐
IV. 93
The synthesis of and 3H labelled methylazoxymethylacetate, ( M A M -OAc) , a hepatotoxic and carcinogenic compound, was accomplished by the incorporation of a radioisotope labelled methyl group into N, N'-dimethylhydrazine with methyl iodide instead oj dimethyl sulfate. Monosodium dibenzoylhydrazine
3H-Sch 47949, racemic 3H-Sch 48461, was prepared at a specific activity of 40 mCi/mmole by Pt catalysed exchange with tritiated water. 3H-Sch 48461 was prepared at a specific activity of 64.6 Ci/mmole by a Pd/C catalysed reduction of an olefinic intermediate. 14C-Sch 48461 was prepared in 8 steps fr