1143534-72-8Relevant articles and documents
Deep learning-driven scaffold hopping in the discovery of Akt kinase inhibitors
Chen, Hongming,Lu, Xiaoyun,Ran, Ting,Song, Shukai,Wang, Zuqin,Wen, Chang,Xu, Fang,Zhou, Yang
, p. 10588 - 10591 (2021/10/19)
Scaffold hopping has been widely used in drug discovery and is a topic of high interest. Here a deep conditional transformer neural network, SyntaLinker, was applied for the scaffold hopping of a phase III clinical Akt inhibitor, AZD5363. A number of nove
A designer axially chiral amino sulfonamide as an efficient organocatalyst for direct asymmetric mannich reactions of N-boc-protected imines
Kano, Taichi,Yamaguchi, Yukako,Maruoka, Keiji
supporting information; experimental part, p. 1838 - 1840 (2009/08/14)
The moderate nucleophilicity of the axially chiral amino sulfonamide (S)-1 suppresses the problematic side reactions, including aldol reactions, in the asymmetric Mannich reaction of N-Boc-protected imines with aldehydes. The corresponding adducts are obtained in good yield and excellent stereoselectivity (see scheme; Boc=tert-butoxycarbonyl, Tf=trifluoromethanesulfonyl).