192725-90-9Relevant articles and documents
Diastereoselective synthesis of novel aza-diketopiperazines via a domino cyclohydrocarbonylation/addition process
Regenass, Pierre,Margathe, Jean-Fran?ois,Mann, André,Suffert, Jean,Hibert, Marcel,Girard, Nicolas,Bonnet, Dominique
supporting information, p. 9657 - 9660 (2014/08/18)
Herein, we report an unprecedented, short and diastereo-selective synthesis of newly reported aza-diketopiperazine (aza-DKP) scaffolds starting from amino acids. The strategy is based on a Rh(i)-catalyzed hydroformylative cyclohydrocarbonylation of allyl-substituted aza-DKP, followed by a diastereoselective functionalization of the platform. This methodology allows the synthesis of novel bicyclic and tricyclic aza-DKP scaffolds incorporating six- or seven-membered rings, with potential applications in medicinal chemistry. This journal is the Partner Organisations 2014.
Pd-catalyzed regioselective allylation of Mono- and disubstituted hydrazines
Tsupova, Svetlana,Maeeorg, Uno
supporting information, p. 3381 - 3383 (2013/07/26)
Palladium-catalyzed allylation of hydrazines using allyl alcohols is reported. This highly efficient protocol furnishes monoallylated hydrazines selectively, in 27-99% yields. Following an optimization of the reaction conditions and of the Pd-ligands, the allylations of both mono- and disubstituted hydrazines were investigated, as well as the effects of C2-substitution on the allylating agent. Of particular interest, a novel method for the selective monoallylation of monosubstituted hydrazines is demonstrated.
N-Boc-O-tosyl hydroxylamine as a safe and efficient nitrogen source for the N-amination of aryl and alkyl amines: Electrophylic amination
Baburaj, Thankappan,Thambidurai, Sivalingam
experimental part, p. 1993 - 1996 (2011/10/08)
β-Boc-protected aryl and alkyl hydrazines, useful intermediates for azapeptides and N-substituted pyrazoles, were synthesized by electrophylic amination methodology, using less energetic N-Boc-O-tosyl hydroxylamine as an efficient nitrogen source. Also we have demonstrated a two-step, chromatography-free synthesis of N-Boc-O-tosyl hydroxylamine. Georg Thieme Verlag Stuttgart - New York.
Use of polyanions for alkylation of hydrazine derivatives
Bredihhin, Aleksei,Maeeorg, Uno
, p. 4975 - 4977 (2008/03/28)
Alkylation of hydrazine and its derivatives still remains a quite complicated task. The novel method utilizing the polyanion strategy is reported. Formation and use of trianion for alkylation of hydrazine derivatives is first reported. Described method pr
NOVEL HETEROCYCLES
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Page/Page column 82, (2010/10/20)
The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
Novel heterocyclic compounds, method for preparing same and use thereof as medicines, in particular as antibacterial agents
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Page/Page column 21, (2010/02/14)
The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds, as well as their use as medicaments, in particular as anti-bacterial agents.
Novel heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors
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, (2008/06/13)
The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and β-lactamase inhibitors.
Retroviral protease inhibiting compounds
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Page 58, (2010/01/31)
A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.
Combination of tert-butoxycarbonyl and triphenylphosphonium protecting groups in the synthesis of substituted hydrazines
Tsubrik, Olga,Maeeorg, Uno
, p. 2297 - 2299 (2007/10/03)
(matrix presented) A new reagent for the systematic synthesis of substituted hydrazines is reported. Unlike previously developed reagents, this one contains only two protecting groups, thus providing a faster approach to multisubstituted derivatives. The selective introduction of alkyl and acyl groups is illustrated by a few examples. Also a new fast method for the deprotection of the triphenylphosphonium group is presented.
RETROVIRAL PROTEASE INHIBITING COMPOUNDS
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, (2008/06/13)
A compound of the formula: STR1 is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.