Synthesis of 3H, 13C, 2H3, 15N and 14C‐labelled SCH 466036, a histamine 3 receptor antagonist. (February 2015)

• Record Type: Journal Article
• Authors: Hesk, D.; Borges, S.; Dumpit, R.; Hendershot, S.; Koharski, D.; Lavey, C.; McNamara, P.; Voronin, K.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 58:Number 2(2015)
• Page Start: 36
• Page End: 41
• Publication Date: 2015-02
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3261
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>The synthesis of [³H]SCH 466036, [Me‐³H₃]SCH 466036, [¹³C, ²H₃, ¹⁵N]SCH 466036 and [¹⁴C]SCH 466036 is described. [³H]SCH 466036 was prepared in two steps via Raney Ni‐catalysed exchange with tritiated water. [Me‐³H₃]SCH 466036 was prepared in a single step from [³H]methyl iodide in 45% yield. [¹³C, ²H₃, ¹⁵N]SCH 466036 was prepared in two steps from [¹⁵N]hydroxylamine and [¹³C, ²H₃]methyl iodide with an overall yield of 16%. [¹⁴C]SCH 466036 was prepared in seven steps from [¹⁴C]potassium cyanide in an overall yield of 13%.</p> </abstract>