1190622-64-0Relevant articles and documents
HFIP Promoted Low-Temperature SNAr of Chloroheteroarenes Using Thiols and Amines
Bhujabal, Yuvraj B.,Vadagaonkar, Kamlesh S.,Gholap, Aniket,Sanghvi, Yogesh S.,Dandela, Rambabu,Kapdi, Anant R.
, p. 15343 - 15354 (2019)
A highly efficient and an unprecedented hexafluoro-2-propanol, promoting low-temperature aromatic nucleophilic substitutions of chloroheteroarenes, has been performed using thiols and (secondary) amines under base-free and metal-free conditions. The developed protocol also provides excellent regio-control for the selective functionalization of dichloroheteroarenes, while the utility of the protocol was demonstrated by the modification of a commercially available drug ceritinib.
Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK)
Trani, Giancarlo,Barker, John J.,Bromidge, Steven M.,Brookfield, Frederick A.,Burch, Jason D.,Chen, Yuan,Eigenbrot, Charles,Heifetz, Alexander,Ismaili, M. Hicham A.,Johnson, Adam,Krülle, Thomas M.,Mackinnon, Colin H.,Maghames, Rosemary,McEwan, Paul A.,Montalbetti, Christian A.G.N.,Ortwine, Daniel F.,Prez-Fuertes, Yolanda,Vaidya, Darshan G.,Wang, Xiaolu,Zarrin, Ali A.,Pei, Zhonghua
, p. 5818 - 5823 (2015/01/08)
Starting from benzylpyrimidine 2, molecular modeling and X-ray crystallography were used to design highly potent inhibitors of Interleukin-2 inducible T-cell kinase (ITK). Sulfonylpyridine 4i showed sub-nanomolar affinity against ITK, was selective versus Lck and its activity in the Jurkat cell-based assay was greatly improved over 2.
