80824-77-7Relevant articles and documents
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics
Huang, Ling,Gao, Lanchang,Zhang, Xiaohua,Yin, Lei,Hu, Jintao,Song, Ting,Chen, Yin
supporting information, (2020/09/01)
We report the optimisation of a series of novel amide-piperidine (piperazine) derivatives using the multiple ligand approach with dopamine and serotonin receptors. Of the derivatives, compound 11 exhibited high affinity for the D2, 5-HT1A, and 5-HT2A receptors, but low affinity for the 5-HT2C and histamine H1 receptors and human ether-a-go-go-related gene (hERG) channels. In vivo, compound 11 reduced apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitching without observable catalepsy, even at the highest dose tested. In addition, it exhibited suppression in a CAR test. Furthermore, in a novel object recognition task, it displayed procognition properties. Therefore, compound 11 is a promising candidate multi-target antipsychotic.
1,2-Benzisoxazol-3-yl Diphenyl Phosphate: A New, Reactive Activating Agent for the Synthesis of Amides, Esters, and Peptides via Condensation
Ueda, Mitsuru,Oikawa, Hideaki
, p. 760 - 763 (2007/10/02)
A new activating agent for condensations, 1,2-benzisoxazol-3-yl diphenyl phosphate (1), was readily prepared in high yield by the reaction of 1,2-benzisoxazol-3-ol (2) with diphenyl phosphorochloridate (3) in the presence of triethylamine in benzene.The reaction of the carboxylic acids with the amines in the presence of 1 was investigated by two procedures, a two-step method and a one-step procedure.Both methods gave the corresponding amides and esters in high yields under mild conditions, but the one-step procedure was found to be superior to the two-step procedure because of its simplicity and speed.Furthermore, the activating agent 1 was shown to be a useful peptide forming reagent.
2(3H)-BENZOXAZOLETHIONE.
Ueda,Kawaharasaki,Imai
, p. 85 - 89 (2007/10/02)
A new condensing agent, N,N prime -carbonyldi left bracket 2(3H)-benzoxazolethione right bracket , was readily prepared by the reaction of 2-benzoxazolethiol and trichloromethyl chloroformate in benzene. The condensing agent is shown to be useful for the preparation of amides, esters, and dipeptides under mild conditions. A successful polyamide synthesis by the polycondensation of isophthalic acid with diamines using the condensing agent is also described.