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Title: Synthesis ofN-(2-chloro-5-methylthiophenyl)-N'-(3-methyl-thiophenyl)-N'-[3H3]methylguanidine, l brace [3H3]CNS-5161 r brace

The preparation of the title compound, [{sup 3}H{sub 3}]CNS-5161, was accomplished in three steps starting with the production of [{sup 3}H{sub 3}]iodomethane (CT{sub 3}I). The intermediate N-[{sup 3}H{sub 3}]methyl-3-(thiomethylphenyl)cyanamide was prepared in 77% yield by the addition of CT{sub 3}I to 3-(thiomethylphenyl)cyanamide, previously treated with sodium hydride. Reaction of this tritiated intermediate with 2-chloro-5-thiomethylaniline hydrochloride formed the guanidine compound [{sup 3}H{sub 3}]CNS-5161. Purification by HPLC gave the desired labeled product in an overall yield of 9% with greater than 96% radiochemical purity and a final specific activity of 66 Ci mmol{sup -1}.
Authors:
; ; ; ;
Publication Date:
OSTI Identifier:
861181
Report Number(s):
LBNL--48958
Journal ID: ISSN 0362-4803; JLCRD4; R&D Project: 366977; BnR: YN0100000; TRN: US0600271
DOE Contract Number:
DE-AC02-05CH11231; NIHP41 RR01237
Resource Type:
Journal Article
Resource Relation:
Journal Name: Journal of Labelled Compounds and Radiopharmaceuticals; Journal Volume: 45; Journal Issue: 5; Related Information: Journal Publication Date: 04/2002
Research Org:
Ernest Orlando Lawrence Berkeley NationalLaboratory, Berkeley, CA (US)
Sponsoring Org:
USDOE Director, Office of Science. Office of Biological andEnvironmental Research. Medical Sciences Division; National Institutes ofHealth
Country of Publication:
United States
Language:
English
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; 62 RADIOLOGY AND NUCLEAR MEDICINE; GUANIDINES; HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY; PRODUCTION; PURIFICATION; SODIUM HYDRIDES; SYNTHESIS CNS-5161 tritium NMDA