Based on the lead compounds 1 and 2, a series of novel BACE1 inhibitors were designed and synthesized,among which compound 9h exhibited a 60 fold improvement in potency over the lead compound 1. This represents a good...Based on the lead compounds 1 and 2, a series of novel BACE1 inhibitors were designed and synthesized,among which compound 9h exhibited a 60 fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD. The result also showed that the prop-2-yn-1-yloxy is a suitable fragment for modification of cyclic acylguanidine BACE1 inhibitors.展开更多
Generation of multi-substituted pyrroles is accomplished through an unexpected iron(Ⅱ)-promoted reaction of N-arylprop-2-yn-1-imines with wate r.This transformation proceeds smoothly with excellent chemoselectivityan...Generation of multi-substituted pyrroles is accomplished through an unexpected iron(Ⅱ)-promoted reaction of N-arylprop-2-yn-1-imines with wate r.This transformation proceeds smoothly with excellent chemoselectivityand regioselectivity.A stoichiometric amount of Fe(OTf)_(2) is necessary for the succes s ful conversion.A Lewis acid-promoted tandem reaction pathway is proposed.展开更多
基金supported by grants from The National Natural Science Foundation of China (No. 81172924)Beijing Municipal Natural Science Foundation (No. 7112106)
文摘Based on the lead compounds 1 and 2, a series of novel BACE1 inhibitors were designed and synthesized,among which compound 9h exhibited a 60 fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD. The result also showed that the prop-2-yn-1-yloxy is a suitable fragment for modification of cyclic acylguanidine BACE1 inhibitors.
基金Financial support from the National Natural Science Foundation of China(Nos.21871053 and 21532001)the Leading Innovative and Entrepreneur Team Introduction Program of Zhejiang(No.2019R01005)is gratefully acknowledged。
文摘Generation of multi-substituted pyrroles is accomplished through an unexpected iron(Ⅱ)-promoted reaction of N-arylprop-2-yn-1-imines with wate r.This transformation proceeds smoothly with excellent chemoselectivityand regioselectivity.A stoichiometric amount of Fe(OTf)_(2) is necessary for the succes s ful conversion.A Lewis acid-promoted tandem reaction pathway is proposed.
