## Abstract The title compound (1) was synthesized by a 7‐step sequence. 4‐Amino‐2‐hydroxy‐[carbonyl‐^14^C]benzoic acid (1) was selectively methylated to provide the ether ester 2, which was smoothly chlorinated in acetic acid to give 3. The ester was hydrolyzed with aqueous potassium hydroxide to
Synthesis of 2–14C-3-amino-1-chloro-5-methylhexan-2-one hydrochloride
✍ Scribed by Neil J. Lewis; Jan Hes; Philip Yip; Frederick D. Cazer
- Publisher
- John Wiley and Sons
- Year
- 1977
- Tongue
- French
- Weight
- 180 KB
- Volume
- 13
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
A convenient synthesis of the ^14^C‐labelled chloromethyl ketone analog of leucine is reported. Modification of previously published conditions allowed for the facile synthesis of: 2–^14^C‐3‐amino‐1‐chloro‐5‐methylhexan‐2‐one hydrochloride in four steps from 1‐^14^C‐DL‐leucine in 85.7% yield. This represented a four‐fold improvement over yields reported previously for compounds of this class.
📜 SIMILAR VOLUMES
## Synthesis of the title compound ( 5 ) . an histamine H2 -receptor antagonist, is described. Treatment of 3-(3-[2.6-C1-piperidinomethylphenoxv)propylamine(l)l with 3-amino-4-methoxy-l,2,5-thiadiazole-1-oxide2 produced 3-amino-4-13-0-[ 2,6-"C]piperidinomethylphenoxy)propylamino~-1,2,5-thiadiazole
## Abstract 7‐Chloro‐1,3‐dihydro‐5‐(2‐fluorophenyl)‐1‐methyl‐2H‐1,4‐benzodiazepin‐2‐one (Fludiazepam) (I), an anti‐anxiety agent, was labelled with carbon‐14 at C‐5 position for metabolic studies. The reaction sequence for the synthesis is shown in Fig. 2. o‐Fluorobenzoic‐^14^C acid (IV) was prepar
Tema~epam-2-'~C, 7-Chloro-1,3-ihydro-3-hydroxy-1 -methyl-5-phenyl-2H-1,4-benzodiazepin-2-one--"C, was prepared in a f ive-step synthesis. Chl~roacetic-l-~~C acid was converted to the acid chloride with thionyl chloride. The acid chloride was allowed to react with 2-methylamino-5-chloro-benzophenone
## Abstract Two benzodiazepines, Diazepam and Flunitrazepam, labeled with carbon‐14 in position 5 of the diazepine ring have been synthesized. Use of a condensation between iminochlorides and ^14^C‐benzonitriles, followed by exhaustive methylation of the resulting quinazolines and hydrolyses is des