17822-51-4Relevant articles and documents
Visible-Light Driven Selective C-N Bond Scission in anti-Bimane-Like Derivatives
Petek, Nejc,Brodnik, Helena,Gro?elj, Uro?,Svete, Jurij,Po?gan, Franc,?tefane, Bogdan
supporting information, p. 5294 - 5298 (2021/06/28)
In the present study, we report the photochemical transformation of pyrazolo[1,2-a]pyrazolone substrates that reach an excited state upon irradiation with visible light to initiate the homolytic C-N bond cleavage process that yields the corresponding N1-s
Facile and innovative catalytic protocol for intramolecular Friedel-Crafts cyclization of Morita-Baylis-Hillman adducts: Synergistic combination of chiral (salen)chromium(III)/ BF3 OEt2 catalysis
Ayyanoth, Karthik Krishna Kumar,Jeyarajan, Helen Ratna Monica,Kamarajapurathu, Raju Subimol,Soundararajan, Karthikeyan
supporting information, p. 2186 - 2193 (2021/09/02)
The chiral (salen)Cr(III)/BF3 OEt2 catalytic combination was found to be an effective catalyst for intramolecular Friedel-Crafts cyclization of electron-deficient Morita-Baylis-Hillman adducts. In presence of mild reaction conditions the chiral (salen)Cr(
Diversity Oriented Clicking (DOC): Divergent Synthesis of SuFExable Pharmacophores from 2-Substituted-Alkynyl-1-Sulfonyl Fluoride (SASF) Hubs
Barrow, Andrew S.,Cheng, Yunfei,Gialelis, Timothy L.,Giel, Marie-Claire,Kitamura, Seiya,Li, Gencheng,Moses, John E.,Ottonello, Alessandra,Sharpless, K. Barry,Smedley, Christopher J.,Wolan, Dennis W.
supporting information, p. 12460 - 12469 (2020/06/10)
Diversity Oriented Clicking (DOC) is a unified click-approach for the modular synthesis of lead-like structures through application of the wide family of click transformations. DOC evolved from the concept of achieving “diversity with ease”, by combining classic C?C π-bond click chemistry with recent developments in connective SuFEx-technologies. We showcase 2-Substituted-Alkynyl-1-Sulfonyl Fluorides (SASFs) as a new class of connective hub in concert with a diverse selection of click-cycloaddition processes. Through the selective DOC of SASFs with a range of dipoles and cyclic dienes, we report a diverse click-library of 173 unique functional molecules in minimal synthetic steps. The SuFExable library comprises 10 discrete heterocyclic core structures derived from 1,3- and 1,5-dipoles; while reaction with cyclic dienes yields several three-dimensional bicyclic Diels–Alder adducts. Growing the library to 278 discrete compounds through late-stage modification was made possible through SuFEx click derivatization of the pendant sulfonyl fluoride group in 96 well-plates—demonstrating the versatility of the DOC approach for the rapid synthesis of diverse functional structures. Screening for function against MRSA (USA300) revealed several lead hits with improved activity over methicillin.