167015-84-1Relevant articles and documents
Combined Approach of Backbone Amide Linking and On-Resin N-Methylation for the Synthesis of Bioactive and Metabolically Stable Peptides
Wesche, Frank,Adihou, Hélène,Kaiser, Astrid,Wurglics, Mario,Schubert-Zsilavecz, Manfred,Kaiser, Marcel,Bode, Helge B.
, p. 3930 - 3938 (2018)
Rhabdopeptides are a large class of nonribosomal peptides from the bacteria Xenorhabdus and Photorhabdus with low micromolar activity against different protozoa, which are the causative agents of several tropical diseases. The development of a facile and flexible synthesis combining backbone amide linking with on-resin peralkylation for the synthesis of permethylated rhabdopeptides is described. This strategy allows the fast generation of permethylated naturally occurring and artificial rhabdopeptides for a structure-activity study. Furthermore, in vitro experiments revealed their superior properties regarding their stability and passive membrane diffusion.
Gold(i)-catalyzed pathway-switchable tandem cycloisomerizations to indolizino[8,7-: B] indole and indolo[2,3-a] quinolizine derivatives
Liu, Chengjun,Sun, Zenghui,Xie, Fukai,Liang, Guoduan,Yang, Lu,Li, Yaqiao,Cheng, Maosheng,Lin, Bin,Liu, Yongxiang
supporting information, p. 14418 - 14421 (2019/12/05)
Experimental and theoretical explorations were performed on the pathways of the cascade cycloisomerizations of tryptamine-N-ethynylpropiolamide substrates. The methodology provided a common strategy to access either indolizino[8,7-b]indoles or indolo[2,3-
INHIBITORS FOR PROLIFERATING CELL NUCLEAR ANTIGEN AND USES
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Paragraph 00135, (2017/07/06)
The present invention relates to series of compounds as an inhibitor targeting Proliferating Cell Nuclear Antigen (PCNA). Pharmaceutical compositions of those compounds and methods of using them in the treatment of cancer are within the scope of this disclosure.
Tandem intramolecular photocycloaddition-retro-mannich fragmentation as a route to spiro[pyrrolidine-3,3′-oxindoles]. Total synthesis of (±)-coerulescine, (±)-horsfiline, (±)-elacomine, and (±)-6-deoxyelacomine
White, James D.,Li, Yang,Ihle, David C.
experimental part, p. 3569 - 3577 (2010/07/04)
Figure presented Irradiation of a tryptamine linked through its side-chain nitrogen to an alkylidene malonate residue results in an intramolecular [2 + 2] cycloaddition to the indole 2,3-double bond. The resultant cyclobutane undergoes spontaneous retro-M
Toward general access to the Aspidosperma-type terpenoid indole alkaloids: Synthesis of the key 3,3-disubstituted piperidones through enantioselective intramolecular Heck-type reaction of chloroformamides
Yasui, Yoshizumi,Takeda, Hiroshi,Takemoto, Yoshiji
experimental part, p. 1567 - 1574 (2009/11/30)
An enantioselective intramolecular Heck-type reaction of chloroformamides has been developed for the synthesis of 3,3-disubstituted piperidones. The desired piperidone was formed in the presence of a palladium catalyst, an optically active phosphoramidite ligand, K3PO4 and Ag 3PO4. The obtained piperidone was converted to epieburnamonine.
Mild and selective deprotection of carbamates with Bu4NF
Jacquemard, Ulrich,Bénéteau, Valérie,Lefoix, Myriam,Routier, Sylvain,Mérour, Jean-Yves,Coudert, Gérard
, p. 10039 - 10047 (2007/10/03)
A new mild method allowing the removal of carbamates using TBAF in THF is reported. Reactions were performed on indole, indoline, N-methyl aniline, aniline and tryptamine derivatives. The observed selectivity according to the carbamates or the substrates is discussed. A mechanism is postulated. Graphical Abstract
New submonomers for poly N-substituted glycines (peptoids)
Uno, Tetsuo,Beausoleil, Eric,Goldsmith, Richard A.,Levine, Barry H.,Zuckermann, Ronald N.
, p. 1475 - 1478 (2007/10/03)
Five protected submonomers for peptoid synthesis were prepared, including N(in)-BOC-tryptamine, O-t-butyl tyramine, PMC-guanidino- propylamine, 6-amino-6-deoxy-D-galactopyranose diacetonide, and 5-amino-2,2- dimethyl-1,3-dioxane. The first three mimic nat
