1563182-47-7Relevant academic research and scientific papers
Nickel/Enamine Cooperative Catalysis Enables Highly Enantioselective Allylic Alkylation of α-Branched Aldehydes
Shen, Hong-Cheng,Zhang, Wen-Qian
, p. 11849 - 11854 (2021/09/28)
All-carbon quaternary stereocenters constitute a significant portion of natural products and bioactive compounds. Here we disclose a nickel and chiral amine cooperative catalysis to enable a highly enantioselective allylic alkylation reaction between α-branched aldehydes and a wide scope of allyl esters, allowing the all-carbon quaternary stereocenter to be accessed with excellent enantioselectivity (up to 98% ee) and structural diversity. The general synthetic applicability has been showcased by the enantioselective synthesis of key chiral building blocks to access (+)-eptazocine, (?)-aphanorphine, and other two bioactive compounds.
Design, synthesis, and optimization of balanced dual NK1/NK 3 receptor antagonists
Hanessian, Stephen,Jennequin, Thomas,Boyer, Nicolas,Babonneau, Vincent,Soma, Udaykumar,Mannoury La Cour, Clotilde,Millan, Mark J.,De Nanteuil, Guillaume
, p. 550 - 555 (2014/06/09)
In connection with a program directed at potent and balanced dual NK 1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pKi values of 8.6 and 8.1, respectively.
