Category: 911705-40-3

Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors was written by Usui, Yoshihiro;Uehara, Fumiaki;Hiki, Shinsuke;Watanabe, Kazutoshi;Tanaka, Hiroshi;Shouda, Aya;Yokoshima, Satoshi;Aritomo, Keiichi;Adachi, Takashi;Fukunaga, Kenji;Sunada, Shinji;Nabeno, Mika;Saito, Ken-ichi;Eguchi, Jun-ichi;Yamagami, Keiji;Asano, Shouichi;Tanaka, Shinji;Yuki, Satoshi;Yoshii, Narihiko;Fujimura, Masatake;Horikawa, Takashi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Electric Literature of C15H20N2O3 The following contents are mentioned in the article:

The results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from authors’ promising compounds containing a 2-phenylmorpholine moiety are described. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on the Ph moiety revealed that a 4-fluoro-2-methoxy group afforded potent inhibitory activity toward GSK-3β. Based on docking studies of (S)-isomer of I, new hydrogen bonding between the nitrogen atom of the piperazine moiety and the oxygen atom of the main chain of Gln185 has been indicated, which may contribute to increased activity compared with that of the corresponding phenylmorpholine analogs. Effect of the stereochem. of the phenylpiperazine moiety is also discussed. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Electric Literature of C15H20N2O3).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Electric Literature of C15H20N2O3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain was written by Chrovian, Christa C.;Soyode-Johnson, Akinola;Ao, Hong;Bacani, Genesis M.;Carruthers, Nicholas I.;Lord, Brian;Nguyen, Leslie;Rech, Jason C.;Wang, Qi;Bhattacharya, Anindya;Letavic, Michael A.. And the article was included in ACS Chemical Neuroscience in 2016.Category: piperazines The following contents are mentioned in the article:

Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound I (huP2X7 IC₅₀ = 9 nM; rat P2X7 IC₅₀ = 42 nM) achieved 80% receptor occupancy for 6 h when dosed orally at 10 mg/kg in rats as measured by ex vivo radioligand binding autoradiog. Structure-activity relationships within this series are described, as well as in vitro ADME results. In vivo pharmacokinetic data for key compounds is also included. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Category: piperazines).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

New intermediates for the selective synthesis of 1-methyl-3-phenylpiperazine and some phenylpiperazine derivatives was written by Rao, Divvela V. N. Srinivasa;Dandala, Ramesh;Handa, Vijay Kumar;Sivakumaran, Meenakshisunderam;Naidu, Andra. And the article was included in ARKIVOC (Gainesville, FL, United States) in 2006.Electric Literature of C15H20N2O3 The following contents are mentioned in the article:

New intermediates 4-protected-1-alkyl-2-oxo-3-phenylpiperazines and 1-alkyl-2-oxo-3-phenylpiperazines for the selective synthesis of 1-alkyl-3-phenylpiperazines, e.g., I, are described. First method involves the reduction of the 4-protected-1-alkyl-2-oxo-3-phenylpiperazines followed by deprotection giving the 1-alkyl-3-phenylpiperazines. Second method involves the deprotection of 4-protected-1-alkyl-2-oxo-3-phenylpiperazines followed by reduction giving the 1-alkyl-3-phenylpiperazines. This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Electric Literature of C15H20N2O3).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Electric Literature of C15H20N2O3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The preparation of 1-Methyl-3-phenylpiperazine was written by Guan, Cheng-bo;Zhang, Xue-mei;Wei, Meng;Lai, Kun-min;Yu, Zhang-xin;Yan, Zhao-hua. And the article was included in Nanchang Daxue Xuebao, Likeban in 2012.Quality Control of tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate The following contents are mentioned in the article:

1-Methyl-3-phenylpiperazine was prepared by using Et α-Bromophenylacetate and ethylenediamine as the starting materials in the cyclization. Then with N₄ protection of the Boc group, N1 methylation, N₄ deprotection and reduction of amide group, 1-Methyl-3-phenylpiperazine was synthesized. The total yield is 29%. On the basis of previously reported procedure, we further modified the work-up procedure in the first step of cyclization to increase the production quality and efficiency. The modification included dissolution of the crude product obtained in CH₂Cl₂, and subsequent reactions with a limited amount of di-tert-butyldicarbonate followed by precipitation in THF at low temperature Our modification improved the quality of the intermediate 3-phenyl-2-piperazinone and is easily repeatable. Moreover, in the steps of N₄ protection with Boc group and reduction of amide group, some changes were also made for easy application to industrial manufacturing This study involved multiple reactions and reactants, such as tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3Quality Control of tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate).

tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate (cas: 911705-40-3) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Quality Control of tert-Butyl 3-oxo-2-phenylpiperazine-1-carboxylate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics