## Abstract Modification of the traditional. Gomberg reaction conditions provides a simple, economical. route to 2‐chlorobiphenyl‐1′,2′,3′,4′,5′,6′‐^14^__C__~6~ __(I). The reaction of benzene‐U‐__^14^__C__~6~ __with an excess of the diasonium salt from__ 2__‐chloroaniline produces__ ^14^__C‐labelle
Synthesis of 2-[4-(diphenylmethyl)-1-piperazinyl]ethyl methyl (±)-1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-[6-14C]pyridinedicarboxylate dihydrochloride ([14C]CV-4093 (2HCl))
✍ Scribed by Norio Tada; Masahiro Kajino; Masazumi Watanabe; Nobuyoshi Hayashi
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 139 KB
- Volume
- 27
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The carbon-I4 labelled compound ( 5 ) of 2-[4-(diphenylmethy1)-l -piperazinyl]ethyl methyl (?)-I ,$-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate dihydrochloride (CV-4093 (2HCI)) was synthesized for the study of its metabolism and distribution in test animals. Starting from the commercially available ethyl[3-' 4C]acetoacetate ( I ), 5 was prepared by a modified Hantzxh synthesis, in an overall radiochemical yield of 23.7%.
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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-
HCl) was synthesized through a straightforward six-step sequence from the readily available [ 14 C-carbonyl]methyl salicylate (2). The overall radiochemical yield of the 1 . 2 HCl from 2 was 10.5%, and its radiochemical purity was 98.8%.
## 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
## Abstract A synthesis of ethyl (__E__)‐4‐[2‐(3,4‐dihydro‐4,4‐dimethyl‐2__H__‐1‐benzopyran‐6‐yl)‐1‐propenyl]benzoate‐__9,10,11,20‐^14^C4__ (1) is described via a multistep procedure similar to that used to obtained the unlabelled compound 2. The latter has shown good activity in several assays com