459174-28-8Relevant academic research and scientific papers
Fine-tuning hydroxylamines as single-nitrogen sources for Pd(0)-catalyzed diamination of o-bromo(or chloro)-biaryls
Ding, Pin,Han, Lingbo,Bai, Jiaxing,Liu, Jingjing,Luan, Xinjun
, p. 686 - 693 (2022/03/19)
Transition metal-catalyzed diamination by hydroxylamines is a common approach for making three-membered aziridines, while its use for building the larger N-heterocycles is still underdeveloped. Herein, we report an efficient Pd(0)-catalyzed inter-molecular [4+1] annulation of o-bromo(or chloro)-biaryls with bifunctional secondary hydroxylamines for the one-step assembly of synthetically useful carbazoles. Noteworthily, a linchpin for this domino reaction was the judicious selection of both the amino-sources and Pd(0)-catalysts for enabling the prerequisite oxidative addition of aryl halides to Pd(0)-species in the presence of hydroxylamines with a labile N-O bond. [Figure not available: see fulltext.].
NEW PIPERIDINYL DERIVATIVES AS INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 7
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, (2019/06/17)
Compounds of formula (I): wherein R1, R2, R3, B, W, Z, m and n are as defined in the description The compounds of the present invention have pro-apoptotic and/ or anti-proliferative properties making it possible to use the
Asymmetric synthesis of 1,2,3-trisubstituted cyclopentanes and cyclohexanes as key components of substance P antagonists
Kuethe, Jeffrey T.,Wong, Audrey,Wu, Jimmy,Davies, Ian W.,Dormer, Peter G.,Welch, Christopher J.,Hillier, Michael C.,Hughes, David L.,Reider, Paul J.
, p. 5993 - 6000 (2007/10/03)
An efficient asymmetric synthesis of 1,2,3-trisubstituted cyclopentanes and cyclohexanes is described. Three methods were developed for the preparation of the 2,3-disubstituted cyclopentenones and cyclohexenones, which are key achiral building blocks. These intermediates are reduced catalytically with (R)-2-methyloxazaborolidine in high yield (82-98%) and excellent ee (89-96%). Directed reduction of the chiral allylic alcohols using Red-Al gives exclusively the 1,2-anti stereochemistry (>99:1). Epimerization of the ester center followed by saponification/crystallization affords the desired hydroxyacids in good yield (65-70%) and in high enantiomeric excess (>99%).
