Poly(ADP-ribose) polymerases (PARPs) are key enzymes in the DNA repair pathway. Inhibitors of these enzymes belong to a new type of anticancer drugs that selectively kill cancer cells by targeting the homologous recombination genetic defects.
Oleh O. Lukianov +4 more
doaj +1 more source
A continuous flow process is presented that couples a Curtius rearrangement step with a biocatalytic impurity tagging strategy to produce a series of valuable Cbz-carbamate products.
Alexander Leslie +4 more
doaj +1 more source
Aim. To synthesize cyclobutane-derived amines and carboxylic acids bearing CH2F or CHF2 groups in the α position; to determine the regularities of the effect of fluoroalkyl substituents on the acid-base properties of the title compounds.
Oleksandr Demchuk, Oleksandr Grygorenko
doaj +1 more source
3,3-dichloro-1,2-diphenylcyclopropene (CPICl)-mediated synthesis of Nα-protected amino acid azides and α-ureidopeptides [PDF]
Rapid synthesis of acid azides via in situ generation of acid chlorides using CPICl as chlorinating agent from the corresponding Nα -protected amino acids is described.
Madhu, C. +3 more
core +4 more sources
Convenient approaches to the synthesis of 6-amino- and 6-oxoimidazo[4,5-b]pyrazolo[3,4-e]pyridines
Aim. To develop convenient approaches to the synthesis of 6-amino- and 6-oxoimidazo[4,5-b]pyrazolo[3,4-e]pyridines as promising biologically active scaffolds. Results and discussion.
Georgiy G. Yakovenko, Mikhailo V. Vovk
doaj +1 more source
The Use of Tetrabutylammonium Azide in the Curtius Rearrangement. [PDF]
Arne Brändström +5 more
openaire +2 more sources
The preparative synthetic approach to α,α-difluoro-γ-aminobutyric acid
Aim. To develop a convenient synthetic approach for the preparation of multigram amounts of 2,2-difluoro-γ-aminobutyric acid, which is pharmacologically promising analog of γ-aminobutyric acid (GABA). Results and discussion.
Maksym Ya. Bugera +3 more
doaj +1 more source
Efficient Synthesis of O-Succinimidyl-(tert-Butoxycarbonylamino)methyl Carbamates Derived from α-Amino Acids Accelerated by Ultrasound: Application to the Synthesis of Ureidodipeptides [PDF]
The synthesis of O-succinimidyl-(tert-butoxycarbonylamino)methyl carbamates employing isocyanates made through the Curtius rearrangement of Boc-amino acid azides in the presence of N-hydroxysuccinimide under the influence of ultrasound is ...
Kantharaju, . +2 more
core +1 more source
Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)-and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine. [PDF]
Various approaches to the synthesis of all four stereoisomers of 2-(1H- imidazol-4-yl)cyclopropylamine (cyclopropylhistamine) are described. The rapid and convenient synthesis and resolution of trans-cyclopropylhistamine is reported.
Appelberg, U. +11 more
core +6 more sources
Ureido Derivatives of Neoabietic Acid
A series of ureido derivatives of neoabietic acid were synthesized by application of Curtius rearrangement reaction to neoabietic acid and amines. Structure characterization of these compounds was done by 1H-NMR, 13C-NMR and HRMS spectral analysis.
Xinyu Gao +4 more
doaj +1 more source

