Journal of Medicinal Chemistry p. 806 - 810 (1984)
Update date:2022-08-04
Topics:
Guan, Ji-Hua
Neumeyer, John L.
Filer, Crist N.
Ahern, David G.
Lilly, Leslie
et al.
The synthesis of the title compounds (1c and its 2H isomer 1b) from N-(2-hydroxyethyl)norapomorphine was carried out by ring bromination, followed by chlorination to the 2-chloroethyl compound 6.Further reduction with 2H2 or 3H2 and Pd/C gave 1b or 1c.Radiochemically pure (97percent) 1c was obtained with a specific activity of 16.3 Ci/mmol.The purity of 1c was determined by LC, HPLC, UV, and NMR. <3H>NCA was shown to label the D2 receptor; however, the D2 signal appears to be only a small portion of the total signal, which may include binding to other dopamine receptor subtypes (D1 and D3).
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