83019-91-4Relevant academic research and scientific papers
tBu4octapa-alkyl-NHS for metalloradiopeptide preparation
Bénard, Fran?ois,Colpo, Nadine,Kuo, Hsiou-Ting,Li, Lily,Lin, Kuo-Shyan,Merkens, Helen,Orvig, Chris,Radchenko, Valery,Schaffer, Paul,Wang, Xiaozhu
, p. 7605 - 7619 (2020/06/21)
The peptide is an important class of biological targeting molecule; herein, a new bifunctional octadentate non-macrocyclic H4octapa,tBu4octapa-alkyl-NHS, which is compatible with solid-phase peptide synthesis and thus usef
Tertiary enamide-promoted diastereoselective domino: N-acyliminium ion trapping and nazarov cyclization
Zheng, Yongxiang,Andna, Lucile,Bistri, Olivia,Miesch, Laurence
supporting information, p. 6771 - 6775 (2020/09/15)
N-Acyliminium ions generated from enamidyl vinyl ketones provided cyclopentenoid-fused diazepines diastereoselectively using BF3·Et2O in one pot through a domino N-acyliminium ion trapping/Nazarov reaction, simultaneously generating three new stereogenic centers. The particular structural design of the cross-conjugated dienone dictates the torquoselectivity observed in this polarized Nazarov reaction. Various N-bridgehead polycyclic scaffolds of putative pharmacological interest were obtained. Cyclic voltammetry was used to support the preferred reaction sequence within this domino reaction.
A DNA-Encoded Chemical Library Incorporating Elements of Natural Macrocycles
Stress, Cedric J.,Sauter, Basilius,Schneider, Lukas A.,Sharpe, Timothy,Gillingham, Dennis
supporting information, p. 9570 - 9574 (2019/06/24)
Here we show a seven-step chemical synthesis of a DNA-encoded macrocycle library (DEML) on DNA. Inspired by polyketide and mixed peptide-polyketide natural products, the library was designed to incorporate rich backbone diversity. Achieving this diversity, however, comes at the cost of the custom synthesis of bifunctional building block libraries. This study outlines the importance of careful retrosynthetic design in DNA-encoded libraries, while revealing areas where new DNA synthetic methods are needed.
Chemoselective alkynylation of N-sulfonylamides versus amides and carbamates-Synthesis of tetrahydropyrazines
Aubineau, Thomas,Cossy, Janine
supporting information, p. 3303 - 3305 (2013/06/04)
The chemoselective alkynylation of N-sulfonylamides versus amides and carbamates using TMS-EBX as an alkynylating agent leads to the formation of non-symmetrical tetrahydropyrazines from orthogonally protected diamines. The Royal Society of Chemistry 2013
C-5 Modified indazolylpyrrolotriazines
-
, (2008/06/13)
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
