1403324-82-2Relevant academic research and scientific papers
Preparation of two D2 partial agonists in C-14 and stable isotope labeled forms
Elmore, Charles S.,Powell, Mark E.,Xiong, Hui,Wu, Ye,Wang, Lijuan,Saunders, David,Urbanek, Rebecca A.
, p. 359 - 365 (2012/11/07)
In support of a program to develop a treatment for diseases resulting from an imbalance in dopamine levels, two drug candidates, 1 and 2, were prepared in stable isotope and C-14 labeled forms. Both compounds contained an aminothiazole ring, and the C-14 label was introduced into the ring using KS14CN. However, the use of KS14CN to form [14C]-2 gave poor results; therefore, benzoyl [14C]isothiocyanate was used instead, which led to a much improved yield. The stable isotope labeled forms were prepared with the label in the side chain from [2H5]ethyl iodide for [2H5]-1 and from 1-[13C]methyl [15N2]pyrazole[13C]carboxaldehyde, which was prepared in turn from [carbonyl-13C]DMF, [15N 2]hydrazine sulfate, and [13C]methyliodide for [ 13C2, 15N2]-2. Copyright
