75946-94-0Relevant articles and documents
Aporphines. 58. N-(2-Chloroethyl)norapomorphine, an Irreversible Ligand for Dopamine Receptors: Synthesis and Application
Guan, Ji-Hua,Neumeyer, John L.,Filer, Crist N.,Ahern, David G.,Lilly, Leslie,et al.
, p. 806 - 810 (2007/10/02)
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. 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).