84226-06-2Relevant articles and documents
Silver(I)-catalyzed iodination of arenes: Tuning the lewis acidity of N-iodosuccinimide activation
Racys, Daugirdas T.,Sharif, Salaheddin A. I.,Pimlott, Sally L.,Sutherland, Andrew
, p. 772 - 780 (2016/02/18)
A mild and rapid method for the iodination of arenes that utilizes silver(I) triflimide as a catalyst for activation of N-iodosuccinimide has been developed. The transformation was found to be general for a wide range of anisole, aniline, acetanilide, and phenol derivatives and allowed the late-stage iodination of biologically active compounds such as PIMBA, a SPECT imaging agent of breast cancer, and (a?)-IBZM, a dopamine D2 receptor antagonist. The method was also modified for the radioiodination of arenes using a one-pot procedure involving the in situ generation of [125I]-N-iodosuccinimide followed by the silver(I)-catalyzed iodination.
RADIOTRACER PRECURSOR AND METHOD FOR PREPARING THE SAME
-
Paragraph 0042; 0043; 0044, (2014/03/25)
A precursor SnBZM for a dopamine receptor radiotracer and a method for preparing the same are revealed. The precursor includes a tributyltin group (Bu3Sn) that is easy to be replaced. Thus a dopamine receptor radiotracer 123I-IBZM ca
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides
de Paulis,Kumar,Johansson,Raemsby,Florvall,Hall,Angeby-Moeller,Ogren
, p. 1263 - 1269 (2007/10/02)
A series of substituted 6-methoxysalicylamides were synthesized from their corresponding 2,6-dimethoxybenzamides by demethylation of one methoxy group with boron tribromide. Substituted 6-methoxysalicylamides having a lipophilic aromatic substituent in the 3-position para with respect to the methoxy group, e.g. a bromo or an iodo atom or an ethyl or a propyl group, and having an (S)-N-(1-alkyl-2-pyrrolidinyl)methyl moiety as the side chain were found to be potent blockers of [3H]spiperone binding in vitro and potent inhibitors of the apomorphine syndrome in the rat. Similar to remoxipride but in contrast to haloperidol, some of the substituted salicylamides show a 10-20 fold separation between the dose that inhibits hyperactivity and that which inhibits stereotypy. It was concluded that, besides the requirement of a lipophilic substitutent in the position para to the methoxy group for antidopamine activity in vivo, the formation of a coplanar six-membered pseudoring involving the amide moiety and the methoxy group is a structural requirement for activity in vitro.