136818-14-9Relevant articles and documents
Method for preparing 1-t-butyloxycarboryl-4-[3-(alkylamino)-2-pyridyl]piperazine
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Paragraph 0072-0078, (2019/06/07)
A method for preparing 1-t-butyloxycarboryl-4-[3-(alkylamino)-2-pyridyl]piperazine belongs to the technical field of organic chemical preparation. The method comprises the following steps: mixing 1-t-butyloxycarboryl-4-(3-nitro-2-pyridyl)piperazine, a catalyst, a cocatalyst and an alkyl ketone, and adding the obtained mixture into an autoclave; sequentially replacing air in the autoclave with nitrogen and hydrogen, continuously introducing hydrogen, and carrying out a reaction; and cooling the reaction system to room temperature, filtering the obtained solution, separating out the obtained lower aqueous layer, drying the obtained upper organic layer, filtering the dried upper organic layer to remove a drying agent, carrying out distillation concentrating, and recrystallizing the obtained concentrate to obtain the target product. The 1-t-butyloxycarboryl-4-(3-nitro-2-pyridyl)piperazine used as a starting material undergoes a reductive alkylation reaction in the presence of the alkyl ketone, the catalyst and hydrogen in the same reactor to obtain the 1-t-butyloxycarboryl-4-[3-(alkylamino)-2-pyridyl]piperazine. The method has the characteristics of simplicity in operation, and high yield.
Oligomer modified diaromatic substituted compounds
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, (2016/01/30)
Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) (PEG) oligome
Strategy for 14C-labeling of a series of bis(heteroaryl) piperazines
Arjomandi, Omid Khalili,Saemian, Nader,Shirvani, Gholamhossein,Javaheri, Mohsen,Esmailli, Kameh
, p. 363 - 366 (2012/06/04)
Four bis(heteroaryl)piperazines labeled with carbon-14 in the 2-position of imidazole moiety were prepared as part of a 4-step (or 5-step) sequence from 5-hydroxymethyl-2-mercapto-1-benzylimida-zole-[2-14C] as a key synthetic intermediate which
Synthesis and anti-HIV-1 activity of new delavirdine analogues carrying arylpyrrole moieties
Pinna,Loriga,Murineddu,Grella,Mura,Vargiu,Murgioni,La Colla
, p. 1406 - 1411 (2007/10/03)
In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) values in the submicromolar range.
Substituted indoles as anti-AIDS pharmaceuticals
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, (2008/06/13)
Substituted indoles of formula (I) STR1 are useful anti-AIDS pharmaceuticals.
Anti-aids piperazines
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, (2008/06/13)
The present invention includes diaromatic substituted heterocyclic compounds (III) STR1 which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors
Romero,Morge,Biles,Berrios-Pena,May,Palmer,Johnson,Smith,Busso,Tan,Voorman,Reusser,Althaus,Downey,So,Resnick,Tarpley,Aristoff
, p. 999 - 1014 (2007/10/02)
A variety of analogues of 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3- (ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead molecule was found to be very sensitive to modifications. Extensive preclinical evaluations of several of these compounds led to the selection of 1-[(5-methoxyindol-2-yl)carbonyl]-4-[3-(ethylamino)-2- pyridyl]piperazine methanesulfonate (U-87201E, atevirdine mesylate) for clinical evaluation.