Journal of medicinal chemistry p. 75 - 79 (1980)
Update date:2022-08-03
Topics:
Vincent
Shambhu
Digenis
A procedure is described for the preparation of [82Br]bromperidol with specific activity 440 muCi/mg. The incorporation of bromine-82 into the molecule was accomplished through Brackman and Smit's modification of the Sandmeyer reaction, during the last step of the synthetic route. This involved the formation of a complex between Cu82Br2 and nitric oxide gas in acetonitrile, which was then allowed to react with 4-[4-(aminophenyl)-4-hydroxy-piperidinyl]-1-(4-fluorophenyl)-1-butanone (aminoperidol, 10) to give [82Br]bromperidol in about 1.5 h. Cupric 82Br]bromide was prepared in situ from K82Br and CuSO4.5H2O. The radiochemical and chemical yields for the preparation of [82Br]bromperidol from K82Br were 10.4 and 12%, respectively. Preliminary tissue distribution studies with the labeled bromperidol in the rat showed that the uptake of radioactivity by the liver, brain, kidneys, and the lungs was very fast and was in the declining phase in the latter organs 15 min after iv administration.
View Morewebsite:http://www.lidepharma.com
Contact:+86-25-58409506
Address:11F, Building A1, No.288 North Zhongshan Road, Gulou District, Nanjing,210003, P.R.China.
Contact:+86-22-26358246
Address:601-4-20, Fujiayuan, Tiantai Road, Hebei District, Tianjin, China
Changzhou Litong Chemical Co., Ltd.
website:http://www.litonchem.com/
Contact:+86-519-86301238
Address:Laoba Rd, Hutang town Changzhou Jiangsu
Chengdu Chengnuo New-Tech Co., Ltd
Contact:0086-028-85749078
Address:4 Jiuyang road,Jiulong industrial port,Chengdu, China
Jiangsu Zhenfang Chemical CO.,LTD.(Suzhou Zhenfang Chemical Factory)
Contact:+86-512-69598882
Address:Room1201, Jiayuan Road No.1018, Xiangcheng District, Suzhou, China
Doi:10.1021/ja9716620
(1997)Doi:10.1016/0040-4020(68)88183-9
(1968)Doi:10.1016/S0957-4166(97)00334-0
(1997)Doi:10.1016/S0022-328X(97)00144-7
(1997)Doi:10.1039/j29680000539
(1968)Doi:10.1021/jo9704568
(1997)