80824-77-7Relevant academic research and scientific papers
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.
3,3'-(Phenylphosphinylidene)bis and 3,3'-(Phenylphosphinylidene)bis. New Activating Agents
Ueda, Mitsuru,Mochizuki, Amane,Hiratsuka, Ichiro,Oikawa, Hideaki
, p. 3291 - 3297 (2007/10/02)
New activating agents, 3,3'-(phenylphophinylidene)bis (4) and 3,3'-(phenylphosphinylidene)bis (5), were readily prepared by the reaction of phenylphosphonic dichloride (3) with 2(3H)-benzoxazolone (1) and 2(3H)-benzothiazolone (2) respectively in the presence of triethylamine at room temperature.The new activating agents 4 and 5 were found to be useful for the preparation of amides, esters, and dipeptides under mild conditions.Furthemore, the direct polycondensation of isophthalic acid with aromatic diamines using the activating agent 4 in the presence of pyridine proceeded fast at room temperature to produce polyamides with inherent viscosities up to 0.80 dL/g.
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.
1,2-BENZISOXAZOL-3(2H)-ONE.
Ueda,Oikawa,Kawaharasaki,Imai
, p. 2485 - 2489 (2007/10/02)
A new condensing agent, N,N prime -carbonyldi left bracket 1,2-benzisoxazol-3(2H)-one right bracket (6), was readily prepared by the reaction of 1,2-benzisoxazol-3-ol and trichloromethyl chloroformate in toluene. The condensing agent 6 was shown to be very useful for the preparation of amides, esters, and dipeptides under mild conditions. A successful polyamide synthesis by one-pot polycondensation of isophthalic acid with diamines using 6 is also described.
THERMOTROPIC LIQUID CRYSTAL BEHAVIOR IN SOME AROMATIC ESTERAMIDES.
Kalyvas,McIntyre
, p. 105 - 118 (2007/10/02)
Ester-amide analogs of p-phenylene di-p-substituted benzoates have been synthesized and the thermotropic liquid crystal properties of the two series are compared. The crystalline, smectic, and nematic phases are all more thermally stable in the ester-amides than in the diesters. In the corresponding series of 4-alkoxybenzoyl compounds, as the alkyl chain length increases the difference in nematic phase stability also increases, but the difference in smectic phase stability decreases. Introduction of a methyl substituent into the central ring reduces the stability of all three phases, and increases the sensitivity of smectic phase stability, but not of crystalline or nematic phase stability, to alkyl chain length.
