- Synthesis of a novel quinoline derivative, 2-(2-methylquinolin-4-ylamino)-N-phenylacetamide - A potential antileishmanial agent
-
Some novel quinoline derivatives were prepared and tested for antileishmanial activity. 2-(2-Methylquinolin-4-ylamino)-N-phenylacetamide (2) was found to be significantly more active than the standard antileishmanial drug sodium antimony gluconate (SAG) i
- Sahu, Niranjan P.,Pal, Chiranjib,Mandal, Nirup B.,Banerjee, Sukdeb,Raha, Mausumi,Kundu, Ashis P.,Basu, Anirban,Ghosh, Monidipa,Roy, Keshab,Bandyopadhyay, Santu
-
-
Read Online
- A crystallographic and solid-state NMR study of 1,4-disubstituted 2,5-diketopiperazines
-
p-Disubstituted phenyldiketopiperazines 1 (R = H), 2 (R = NO2) and 3 (R = -N(CH3)2) were synthesized and characterized by NMR in solution and IR spectroscopy. The identity of the compounds was confirmed and their fragmenta
- Peri?, Berislav,Juraj, Natalija Pantalon,Szalontai, Gábor,Veli?kovi?, Suzana R.,Veljkovi?, Filip M.,Viki?-Topi?, Dra?en,Kirin, Sre?ko I.
-
-
Read Online
- A study of diketopiperazines as electron-donor initiators in transition metal-free haloarene-arene coupling
-
Several diketopiperazines have been shown to promote carbon-carbon coupling between benzene and aryl halides in the presence of potassium tert-butoxide and without the assistance of a transition metal catalyst. The structure of the diketopiperazine has an influence on its reductive potential and can help to promote the coupling of the more challenging aryl bromides with benzene.
- Cumine, Florimond,Zhou, Shengze,Tuttle, Tell,Murphy, John A.
-
p. 3324 - 3336
(2017/04/21)
-
- The cytotoxic effects of diketopiperaizes against Leishmania donovani promastigotes and amastigotes
-
A series of diketopiperazine derivatives (1-12) were evaluated for their in vitro cytotoxic activity against Leishmania donovani promastigotes and amastigotes. Cytotoxicity study revealed that the number and types of the substituents in the phenyl rings h
- Maity, Arindam,Hazra, Abhijit,Palit, Partha,Mondal, Shymal,Lala, Sanchaita,Mondal, Nirup B.
-
p. 3452 - 3458
(2013/07/19)
-
- Efficient synthesis of piperazinediones using potassium iodide catalysis in aqueous media
-
A simple and efficient synthetic approach to 1,4-disubstituted piperazine-2,5-diones was developed. A series of symmetrical 1,4-disubstituted piperazine-2,5-diones was prepared from chloroacetamides using potassium iodide catalysis in acetone/water. The structures of two products were confirmed by single crystal X-ray diffraction analysis.
- Wen, Yong-Hong,Chen, Xiao-Na,Wen, Hui-Ling,Tang, Xiao-Fang
-
experimental part
p. 732 - 736
(2012/06/01)
-
- One-step diketopiperazine synthesis using phase transfer catalysis
-
A simple and efficient one-step procedure is described for the synthesis of a number of symmetrical 1,4-disubstituted piperazine-2,5-diones under phase transfer conditions. The reactions are carried out at room temperature, starting from a suitable N-chloroacetamide in the presence of an aqueous solution of sodium hydroxide. Piperazine-2,5-diones were obtained with excellent selectivity in yields of up to 90%.
- O'Reilly, Elaine,Lestini, Elena,Balducci, Daniele,Paradisi, Francesca
-
experimental part
p. 1748 - 1750
(2009/07/05)
-
- Synthesis of 1,4-diaryl-piperazine-2,5-diones: New behavior of N,N-dimethylformamide dimethyl acetal (DMFDMA)
-
Reactions of chloroacetamides (5) with N,N-dimethylformamide dimethyl acetal gave 1,4-diaryl-piperazine-2,5-diones 11a-e in good yield, rather than 1,5-diaryl-3,7-dimethoxy-1H,5H-[1,5]diazocine-2,6-diones (9a-e). Copyright Taylor & Francis Group, LLC.
- Abu-Shanab, Fathi A.,Al-Harrasi, Ahmed,Mousa, Sayed A. S.
-
p. 376 - 382
(2008/04/01)
-
- Synthesis of symmetrically 1,4-disubstituted piperazine-2,5-diones: A new class of antileishmanial agents
-
A series of 1,4-diphenyl-2,5-dioxopiperazine derivatives were synthesised in one pot sequence. The compounds demonstrated appreciable cytotoxic activity against Leishmania donovani on both forms of the parasite, and the results suggested that some derivat
- Hazra, Abhijit,Paira, Priyankar,Palit, Partha,Banerjee, Sukdeb,Mondal, Nirup B.,Sahu, Niranjan P.
-
p. 381 - 383
(2008/02/11)
-
- Electrochemical Studies on Haloamides. Part 4. Reactivity of Haloacetamides and Haloacetohydroxamates Toward Electrogenerated Diethyl Malonate Anion
-
The reactivity of haloacetamides and acetohydroxamates 1 and 2 toward electrogenerated diethyl malonate anion has been investigated.The course of the reaction primarily depends on the acidity of the amide NH group, which is mainly determined by the nature of the substituent, R, at the nitrogen atom.If this substituent is the same, the nature of the halogen atom also plays an important role.If the malonate anion can act as a base, products arising from follow-up reactions of the conjugated base of the substrate are formed and their structure is dependent on R.In particular, β-lactams arising from a formal insertion of a malonate residue into the amide skeleton are obtained from haloacetanilides.When the substrate cannot be deprotonated, the diethyl malonate anion behaves as a nucleophile provided that the leaving group is bromide.Chloro derivatives are rather stable toward malonate anion.
- Casadei, Maria Antonietta,Rienzo, Barbara Di,Inesi, Achille,Moracci, Franco Micheletti
-
p. 379 - 382
(2007/10/02)
-
- Electrochemical Studies on Haloamides. Part 3. Haloacetamides and Haloacetohydroxamates
-
The electrochemical reduction of haloacetamides and acetohydroxamates 1 and 2 at a mercury cathode in DMF-0.1 mol dm-3 TEAP (tetraethylammonium perchlorate) solutions has been investigated.The reduction leads to the corresponding dehalogenated products together with cyclic dimers, arising from follow-up reactions of the conjugated base of the starting compound.The same type of products, but in quite different yield, are formed when ethyl isobutyrate anion is electrogenerated in the presence of chloro derivatives 1.The reactivity of the substrates, and in particular the structure of the dimers, primarily depends on the nature of the substituent at the amide nitrogen.Possible reaction pathways leading to the products are suggested.
- Casadei, Maria Antonietta,Rienzo, Barbara Di,Inesi, Achille,Moracci, Franco Micheletti
-
p. 375 - 378
(2007/10/02)
-
- Convenient Syntheses of Cyclic Carboxamides from α,β,γ,δ and ε-halocarboxamides under Phase Transfer Conditions
-
Piperazine-2,5-diones (2) were prepared by N-alkylation between two molecules of α-halocarboxamides (1) in the presence of a phase transfer catalyst in yields of 64-88percent. β,γ,δ and ε-Lactams (6,9 and 13) were similarly synthesized by intramolecular N-alkylation of the corresponding halocarboxamides (5, 8 and 12) under phase transfer conditions in 53-99percent yields.Keywords--piperazine-2,5-dione; β-lactam; γ, δ, and ε lactams; bis-β-lactam; phase transfer catalyst; intramolecular N-alkylation
- Okawara, Tadashi,Matsuda, Takashi,Furukawa, Mitsuru
-
p. 1225 - 1233
(2007/10/02)
-
- Base-promoted Reactions of α-Halogeno-alkylanilides
-
Hydride-promoted reactions of 2-halogeno-alkylcarboxanilides afford heterocyclic and acyclic condensation products, some of the latter compounds arising upon hydrolysis and/or rearrangement of the former ones.Competitive formation of dioxopiperazines versus oxazolidinone derivatives or their transformation products depends mainly upon the nature (primary, secondary or tertiary) of the halide moiety.Concurrent dehydrohalogenation of 2-bromo-isobutyranilides leads to unsaturated condensation products.
- Cavicchioni, Giorgio,Scrimin, Paolo,Veronese, Augusto C.,Balboni, Gianfranco,D'Angeli, Ferruccio
-
p. 2969 - 2972
(2007/10/02)
-
- CONVENIENT SYNTHESES OF PIPERAZINE-2,5-DIONES AND LACTAMS FROM HALOCARBOXAMIDES USING PHASE TRANSFER CATALYSTS
-
Inter- and intramolecular N-alkylation of α-halocarboxamides and dihalocarboxamides in the presence of solid phase transfer catalyst led to the corresponding piperazine-2,5-diones (2) and lactams (4) in the yields of 64-88 and 63-99 percent, respectively.A one-pot synthesis of β-lactams (7) from α-methyl-α,β-dibromopropionyl chloride (5) and α-amino acid using phase transfer catalyst was also successfully achieved.
- Okawara, Tadashi,Noguchi, Yoshihide,Matsuda, Takashi,Furukawa, Mitsuro
-
p. 185 - 188
(2007/10/02)
-