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

Journal Article · Fri Sep 28 00:00:00 EDT 2001 · Journal of Labelled Compounds and Radiopharmaceuticals

OSTI ID:861181

Gibbs, Andrew R; Morimoto, Hiromi; VanBrocklin, Henry F; Williams, Philip G; Biegon, Anat

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}.

• Research Organization: Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States)
• Sponsoring Organization: USDOE Director, Office of Science. Office of Biological andEnvironmental Research. Medical Sciences Division; National Institutes ofHealth
• DOE Contract Number: DE-AC02-05CH11231; NIHP41 RR01237
• OSTI ID: 861181
• Report Number(s): LBNL-48958; JLCRD4; R&D Project: 366977; BnR: YN0100000; TRN: US0600271
• Journal Information: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 45, Issue 5; Related Information: Journal Publication Date: 04/2002; ISSN 0362-4803
• Country of Publication: United States
• Language: English

Related Subjects

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