145208-86-2Relevant articles and documents
Vibrational spectrum of buspirone
Cybulski, Jacek,Chilmonczyk, Zdzislaw,Glice, Magdalena,Cybulski, Marcin,Bajdor, Krzysztof,Les, Andrzej
, p. 221 - 234 (1997)
The IR and Raman spectra of buspirone and buspirone hydrochloride were recorded in KBr pellets and chloroform solutions. Most of the vibrational bands were assigned to normal modes using quantum mechanical semiempirical and ab initio restricted Hartree-Fock (RHF) calculations on model systems. The essential spectral characteristics can be obtained from the analysis of three building blocks of buspirone, i.e. pyrimidine-piperazine, butyl spacer and imide residues. The spectral regions particularly sensitive to intermolecular interactions were identified. The theoretical calculations suggest that the 'NH+' band in buspirone hydrochloride reflects the formation of a moderately strong hydrogen bond between the protonated piperazine nitrogen atom (bound to the butyl spacer) and the chlorine anion.
Palladacycle-Phosphine Catalyzed Methylation of Amines and Ketones Using Methanol
Mamidala, Ramesh,Biswal, Priyabrata,Subramani, M. Siva,Samser, Shaikh,Venkatasubbaiah, Krishnan
, p. 10472 - 10480 (2019/08/20)
Methylation of amines and ketones with palladacycle precatalyst has been performed using methanol as an environmentally benign reagent. Various ketones and amines undergo methylation reaction to yield monomethylated amines or ketones in moderate to good isolated yields. Moreover, this protocol was tested for the chemoselective methylation of 4-aminobenzenesulfonamide. The scope of the reaction was further extended to the deuteromethylation of ketones.
Commercial Pd/C-Catalyzed N-Methylation of Nitroarenes and Amines Using Methanol as Both C1 and H2 Source
Goyal, Vishakha,Gahtori, Jyoti,Narani, Anand,Gupta, Piyush,Bordoloi, Ankur,Natte, Kishore
, p. 15389 - 15398 (2019/12/04)
Herein, we report commercially available carbon-supported-palladium (Pd/C)-catalyzed N-methylation of nitroarenes and amines using MeOH as both a C1 and a H2 source. This transformation proceeds with high atom-economy and in an environmentally friendly way via borrowing hydrogen mechanism. A total of >30 structurally diverse N-methylamines, including bioactive compounds, were selectively synthesized with isolated yields of up to 95%. Furthermore, selective N-methylation and deuteration of nimesulide, a nonsteroidal anti-inflammatory drug, were realized through the late-stage functionalization.
Piribedil preparation method
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Paragraph 0012; 0013; 0014; 0015, (2017/07/21)
The invention provides a piribedil preparation method which is characterized in that N-Methylpiperazine, 2-hydroxypyrimidine and 4-Bromo-1,2-(methylenedioxy)benzene are used as raw materials, reaction steps are short, reaction conditions are mild, side reactions in the reaction process are few, and purity of a finished product is high. The process is simple in operation, and the preparation process is little in pollutant emission, little in pollution and is favorable for environment protection.
Aminomethylation via cyclopalladated-ferrocenylimine-complexes-catalyzed Suzuki-Miyaura coupling of aryl halides with potassium N, N - dialkylaminomethyltrifluoroborates
Zou, Dapeng,Cui, Hongmeng,Qin, Lijin,Li, Jingya,Wu, Yangjie,Wu, Yusheng
scheme or table, p. 349 - 356 (2011/03/23)
Using cyclopalladated ferrocenylimine complexes (1-3 mol%) as catalysts, the Suzuki-Miyaura coupling of potassium N,N-dialkylaminomethyltrifluoroborates with aryl and heteroaryl halides were carried out in a 10:1 THF-H2O mixture at 80° in the presence of Cs2CO3 (3.0 equiv) as base, giving the desired cross-coupling products in 14-87% yields. A variety of potassium alkyltrifluoroborates were also examined. Georg Thieme Verlag Stuttgart New York.
Hybridized and isosteric analogues of N1-acetyl-N4-dimethyl-piperazinium iodide (ADMP) and N1-phenyl-N4-dimethyl-piperazinium iodide (DMPP) with central nicotinic action
Manetti, Dina,Bartolini, Alessandro,Borea, Pier Andrea,Bellucci, Cristina,Dei, Silvia,Ghelardini, Carla,Gualtieri, Fulvio,Romanelli, Maria Novella,Scapecchi, Serena,Teodori, Elisabetta,Varani, Katia
, p. 457 - 465 (2007/10/03)
A series of piperazine derivatives, obtained by hybridization of N1-acetyl-N4-dimethyl-piperazinium iodide (1, ADMP) and N1-phenyl-N4-dimethyl-piperazinium iodide (3, DMPP) or of the corresponding tertiary bases (2, 4) with arecoline (5) and arecolone (6) or by isosteric substitution of the phenyl ring of DMPP, has been synthesized. Hybridization afforded compounds that, both as tertiary bases and as iodomethylates, have no affinity for the nicotinic receptor. On the contrary, isosteric substitution gave compounds that maintain affinity for the receptor; among them, two tertiary bases (37, 38), show affinity in the nanomolar range for the nicotinic receptor. The pharmacological profile of these isomeric compounds is quite interesting as they present differences in their peripheral and central effects, suggesting that they interact with different subtypes of the nicotinic receptor. Copyright (C) 1999 Elsevier Science Ltd.
Structure-activity relationship studies of CNS agents. Part 14: Structural requirements for the 5-HT(1A) and 5-HT(2A) receptor selectivity of simple 1-(2-pyrimidinyl)piperazine derivatives
Mokrosz,Strekowski,Duszynska,Harden,Mokrosz,Bojarski
, p. 801 - 806 (2007/10/02)
The 5-HT(1A) and 5-HT(2A) receptor affinity of model 1-(2-pyrimidinyl)-piperazine derivatives 15-21 and 23-32 has been determined. 2-(N-Methylpiperazino)-4,6-di(2-thienyl)pyrimidine 26 is a new, highly active and selective 5-HT(2A) receptor ligand. The to
