30391-55-0Relevant academic research and scientific papers
Mechanochemical N-alkylation of imides
Bri?, Anamarija,Dud, Mateja,Margeti?, Davor
supporting information, p. 1745 - 1752 (2017/09/27)
The mechanochemical N-alkylation of imide derivatives was studied. Reactions under solvent-free conditions in a ball mill gave good yields and could be put in place of the classical solution conditions. The method is general and can be applied to various imides and alkyl halides. Phthalimides prepared under ball milling conditions were used in a mechanochemical Gabriel synthesis of amines by their reaction with 1,2-diaminoethane.
New arylpiperazines with flexible versus partly constrained linker as serotonin 5-HT1A/5-HT7 receptor ligands
Kowalski, Piotr,Mitka, Katarzyna,Jaskowska, Jolanta,Duszynska, Beata,Bojarski, Andrzej J.
, p. 339 - 348 (2013/07/19)
A series of new long-chain arylpiperazine (LCAP) derivatives with flexible and partly constrained alkyl linker were synthesized and investigated in vitro as potential serotonin 5-HT1A and 5-HT7 receptor ligands. The compounds were prepared by a two-step procedure using naphthalimide and 2H-1,3-benzoxazine-2,4(3H)-dione as imides, and 1-(2-methoxyphenyl)piperazine (o-OMe-PhP) and 1,2,3,4-tetrahydroisoquinoline (THIQ) as amine pharmacophores. Modifications of the spacer structure included introduction of flexible penta- and hexamethylene chains as well as partly constrained m- and p-xylyl moieties. In general, the new compounds were more active at the 5-HT1A than at the 5-HT7 receptor, and the o-OMe-PhP derivatives displayed higher affinities than their respective THIQ analogs. The spacer modifications had little effect on the observed in vitro activities. Within the o-OMe-PhP series, except for a small binding reduction for ligands containing the m-xylyl moiety, there was no substantial change in the compounds' potency at both receptors, while for the THIQ derivatives a clear structure-activity relationship was visible only for the interaction of the compounds with the 5-HT7 receptor, which strongly favored flexible analogs. New LCAP derivatives with flexible and partly constrained alkyl linker were tested as potential serotonin 5-HT1A and 5-HT7 receptor ligands. The spacer structure was modified by introduction of flexible penta- and hexamethylene chains and partly constrained m- and p-xylyl moieties. The new compounds were more active at the 5-HT1A than at the 5-HT7 receptor. o-OMe-PhP derivatives displayed higher affinities than their respective THIQ analogs. The spacer modifications had little effect on the observed in vitro activities. Copyright
