26108-53-2Relevant academic research and scientific papers
Catalytic Formal Hydroamination of Allylic Alcohols Using Manganese PNP-Pincer Complexes
Duarte de Almeida, Leandro,Bourriquen, Florian,Junge, Kathrin,Beller, Matthias
, p. 4177 - 4181 (2021/03/26)
Several manganese-PNP pincer catalysts for the formal hydroamination of allylic alcohols are presented. The resulting γ-amino alcohols are selectively obtained in high yields applying Mn-1 in a tandem process under mild conditions. (Figure presented.).
Anti-Markovnikov Hydroamination of Racemic Allylic Alcohols to Access Chiral γ-Amino Alcohols
Liu, Haoying,Sun, Huaming,Tang, Weijun,Wang, Chao,Wang, Kun,Xiao, Jianliang,Xu, Ruirui,Xue, Dong
supporting information, p. 21959 - 21964 (2020/10/06)
A ruthenium-catalyzed formal anti-Markovnikov hydroamination of allylic alcohols for the synthesis of chiral γ-amino alcohols is presented. Proceeding via an asymmetric hydrogen-borrowing process, the catalysis allows racemic secondary allylic alcohols to react with various amines, affording enantiomerically enriched chiral γ-amino alcohols with broad substrate scope and excellent enantioselectivities (68 examples, up to >99 % ee).
Cobalt-Catalyzed Diborylation of 1,1-disubstituted Vinylarenes: A Practical Route to Branched gem-Bis(boryl)alkanes
Teo, Wei Jie,Ge, Shaozhong
supporting information, p. 1654 - 1658 (2018/01/15)
We report the first catalytic diborylation of 1,1-disubstituted vinylarenes with pinacolborane using a cobalt catalyst generated from bench-stable Co(acac)2 and xantphos. A wide range of 1,1-disubstituted vinylarenes underwent this transformati
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents
Chae, Eunhee,Yi, Hanju,Choi, Yeonjung,Cho, Hyeon,Lee, Kiho,Moon, Hongsik
scheme or table, p. 2434 - 2439 (2012/05/05)
A series of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives were synthesized through discovery strategies for balancing target-based in vitro screening and phenotypic in vivo screening. All the newly synthesized compounds were
NOVEL CARBAMOYLOXY ARYL ALKAN ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND
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Page/Page column 49-50, (2009/01/20)
There is provided a novel carbamoyloxy arylalkan arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Ibrmula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction
Kolasa, Teodozyj,Matulenko, Mark A.,Hakeem, Ahmed A.,Patel, Meena V.,Mortell, Kathleen,Bhatia, Pramila,Henry, Rodger,Nakane, Masaki,Hsieh, Gin C.,Terranova, Marc A.,Uchic, Marie E.,Miller, Loan N.,Chang, Renje,Donnelly-Roberts, Diana L.,Namovic, Marian T.,Hollingsworth, Peter R.,Martino, Brenda,El Kouhen, Odile,Marsh, Kennan C.,Wetter, Jill M.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
, p. 5093 - 5109 (2007/10/03)
A new series of dopamine D4 receptor agonists, 1-aryl-3-(4-pyridinepiperazin-1-yl)propanone oximes, was designed through the modification of known dopamine D4 receptor agonist PD 168077. Replacement of the amide group with a methylene-oxime moiety produced compounds with improved stability and efficacy. Structure-activity relationsips (SAR) of the aromatic ring linked to the N-4-piperazine ring confirmed the superiority of 2-pyridine as a core for D4 agonist activity. A two-methylene linker between the oxime group and the N-1-piperazine ring displayed the best profile. New dopamine D4 receptor agonists, exemplified by (E)-1-(4-chlorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime (59a) and (E)-1-(3-chloro-4-fluorophenyl)-3-(4-pyridin-2- ylpiperazin-1-yl)propan-1-one O-methyloxime (64a), exhibited favorable pharmacokinetic profiles and showed oral bioavailability in rat and dog. Subsequent evaluation of 59a in the rat penile erection model revealed in vivo activity, comparable in efficacy to apomorphine. Our results suggest that the oximes provide a novel structural linker for 4-arylpiperazine-based D 4 agonists, possessing leadlike quality and with potential to develop a new class of potent and selective dopamine D4 receptor agonists.
SEROTONIN REUPTAKE INHIBITORS
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Page/Page column 9, (2010/02/14)
A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT,such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.
Oximes and hydrazones that are useful in treating sexual dysfunction
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Page/Page column 35, (2010/02/13)
The present invention relates to oximes and hydrazones of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
Hypolipidemic effects of α, β, and γ-alkylaminophenone analogs in rodents
Huang,Hall
, p. 281 - 290 (2007/10/03)
A number of N-substituted β-alkylaminophenone derivatives including two (α- and two γ-alkylaminophenone analogs were synthesized and investigated for hypolipidemic activity in mice at 8 mg/kg/day ip. Most of these analogs were found to be significantly more active than lovastatin and clofibrate. N-Phenylpiperazinopropiophenone 16 was one of the best derivatives, lowering serum cholesterol levels 41% and serum triglyceride levels 48% after 16 days of drug administration in CF1 mice. In Sprague-Dawley rats, N-phenylpiperazinopropiophenone at 8 mg/kg/day orally also demonstrated more potent hypolipidemic activity than clofibrate, gemfibrozil, and lovastatin at their therapeutic dosage. It significantly reduced tissue cholesterol and triglyceride levels in the aorta wall tissue and lowered the cholesterol and triglyceride levels in chylomicron, very low density lipid (VLDL) and low density lipid (LDL) fractions, while it significantly elevated the cholesterol levels in high density lipid (HDL) fraction. This compound also proved to be active in lowering both cholesterol and triglyceride levels in hyperlipidemic mice and rats induced with atherogenic diet. In vitro liver acetyl coenzyme A (CoA) synthetase, 3-hydroxy-3-methyl glutaryl (HMG) CoA reductase, acyl CoA cholesterol acyl transferase (ACAT), sn-glycerol-3-phosphate acyltransferase, phosphatidylate phosphohydrolase, and hepatic lipoprotein lipase activities were significantly inhibited by N-phenylpiperazinopropiophenone from 25 to 100 μM.
Synthesis of 3-aryloxy-3-phenylpropanamines as possible antidepressants
Sharma. V. L.,Bhandari, Kalpana,Chatterjee, S. K.,Satyanarayana, K. V.,Dua, P. R.
, p. 393 - 396 (2007/10/02)
Thirteen new 3-aryloxy-3-phenylpropanamines (11-23) have been prepared and their structures elucidated by mass, IR and 1H-NMR spectra and by elemental analysis.Being structurally similar to fluoxetine these compounds have been tested for their effect on g
