15854-75-8Relevant articles and documents
1-CYANO-PYRROLIDINE DERIVATIVES AS INHIBITORS OF USP30.
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Page/Page column 60, (2018/02/03)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylatingenzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein R1, R 2, R 3, m, L and X are as defined herein.
Chelation-assisted cross-coupling of anilines through in situ activation as diazonium salts with boronic acids under ligand-, base-, and salt-free conditions
Joncour, Roxan,Susperregui, Nicolas,Pinaud, Noel,Miqueu, Karinne,Fouquet, Eric,Sotiropoulos, Jean-Marc,Felpin, Francois-Xavier
, p. 9291 - 9296 (2013/07/26)
We describe the coupling of anilines with aryl boronic acids, under ligand-, base-, and salt-free conditions at room temperature. This new reaction proceeds through the formation of an aryl palladium alkoxo complex, which allows the transmetalation step w
Cross-coupling of triallyl(aryl)silanes with aryl bromides and chlorides: An alternative convenient biaryl synthesis
Sahoo, Akhila K.,Oda, Takuro,Nakao, Yoshiaki,Hiyama, Tamejiro
, p. 1715 - 1727 (2007/10/03)
Cross-coupling of a diverse range of aryl bromides with triallyl(aryl)silanes is effective in the presence of PdCl2/PCy 3 and tetrabutylammonium fluoride (TBAF) in DMSO-H2O to give various biaryls in good yields. It is worthwhile to note that the all-carbon-substituted arylsilanes, stable towards moisture, acid, and base and easily accessible, serve as a highly practical alternative to their aryl(halo)silane counterparts. A catalyst system consisting of [η3-C3H5)PdCl]2 and 2-[2,4,6-(i-Pr)3C6Ha]-C6H4PCy 2 and use of TBAF· 3 H2O in THF-H2O are effective especially for the cross-coupling with aryl chlorides. Both of the catalyst systems tolerate a broad spectrum of common functional groups. The high efficiency of reactions is presumably due to the ready cleavage of the allyl groups upon treatment with TBAF·3 H2O and an appropriate amount of water. Diallyl(diphenyl)silane also cross-couples with various aryl bromides and chlorides in good yields, whereas allyl(triphenyl)silane gives the cross-coupled products in only moderate yields. Through sequential cross-coupling of bromochlorobenzenes with different arylsilanes, a range of unsymmetrical terphenyls are accessible in good overall yields.
New non peptidic C5a receptor antagonists
Astles, Peter C.,Brown, Thomas J.,Cox, Paul,Halley, Frank,Lockey, Peter M.,McCarthy, Clive,McLay, Iain M.,Majid, Tahir N.,Morley, Andrew D.,Porter, Barry,Ratcliffe, Andrew J.,Walsh, Roger J.A.
, p. 907 - 912 (2007/10/03)
A series of phenylguanidines which bind to the C5a receptor has been developed. The lead compound 1 (IC50 = 30 μM), discovered through random screening, has been modified to provide 32 (RPR121154) with submicromolar activity. This compound was