Journal of labelled compounds and radiopharmaceuticals p. 447 - 456 (1999)
Update date:2022-08-03
Topics:
Schoenbaechler, Roland
Ametamey, Simon M.
Schubiger, Pius A.
The synthesis and 11C-radiolabelling of a new tropane analogue, 3β-(4'-chlorophenyl)-2β-(3'-phenylisoxazol-5'-yl)tropane (β-CPPIT), an inhibitor of the dopamine transporter, is reported. The desmethyl compound, 3β-(4'-chlorophenyl)-2β-(3'-phenylisoxazol-5'-yl)nortropane (5) was prepared via a six-step reaction sequence starting from cocaine. [11C]-β-CPPIT was labelled by N-methylation using [11C]-methyl iodide obtained from the gas phase reaction of [11C]-methane with iodine in 60 +/- 10 percent radiochemical yield (decay corrected from [11C]-methyl iodide). The overall synthesis time was on average 60 minutes at EOB (end of bombardment). The final product had a specific activity of 2000 - 2700 Ci/mmol (74 - 100 TBq/mmol) at EOS (end of synthesis) and the radiochemical purity was greater than 99 percent. [11C]-β-CPPIT showed a logP value of 2.1 indicating that a free diffusion through the blood-brain-barrier should be possible.
View MoreTianjin Te-An Chemtech Co., Ltd.(expird)
Contact:+86-22-65378638
Address:A5-8, No.80 Haiyun Street, TEDA
Yuan Shi(SuQian)Biotechnology Co.,Ltd
website:http://www.yuanshibio.com
Contact:+86-527-84226672
Address:jiangsu suqian
Hangzhou Eastbiopharm Co.,Ltd.
Contact:+86-571-88931780
Address:Hangzhou,China
Chengdu Aslee Biopharmaceuticals, Inc
Contact:18608018419
Address:Chengdu Aslee Biopharmaceuticals, Inc
KA-SHING Business Trade Macau Co., Ltd.
Contact:00853-28430045
Address:23rd Floor, Block 3 La Cite, Areia Preta, Macao
Doi:10.1055/s-2002-19769
(2002)Doi:10.1021/jo001101i
(2000)Doi:10.1007/BF00908206
()Doi:10.1016/S0020-1693(99)00081-X
(1999)Doi:10.1016/S0968-0896(00)00054-7
(2000)Doi:10.1002/ardp.19582910106
(1958)