3989-13-7Relevant articles and documents
Design and synthesis of 3′-(prop-2-yn-1-yloxy)-biphenyl substituted cyclic acylguanidine compounds as BACE1 inhibitors
Liu, Jia-Kuo,Gu, Wei,Cheng, Xiao-Rui,Cheng, Jun-Ping,Nie, Ai-Hua,Zhou, Wen-Xia
, p. 961 - 963 (2016)
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 promi
(3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative as well as preparation method and application thereof
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Paragraph 0147, (2021/08/07)
The invention relates to the technical field of medicinal chemistry, and discloses a (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative derivative as shown in a formula X which is described in the specification. The derivative has good and broad-spec
Catalytic Activation of Trimethylsilylacetylenes: A One-Pot Route to Unsymmetrical Acetylenes and Heterocycles
Lasányi, Dániel,Mészáros, ádám,Novák, Zoltán,Tolnai, Gergely L.
, p. 8281 - 8291 (2018/06/11)
For the synthesis of unsymmetrical acetylenes, a Sonogashira coupling-deprotection-Sonogashira coupling reaction sequence is often used. Removal of protecting groups requires harsh conditions or an excess of difficult to handle and expensive reagents. Herein, we disclose a novel catalytic method for the selective deprotection of trimethylsilylacetylenes in Sonogashira reaction. The reagent hexafluorosilicic acid, an inexpensive nontoxic compound, was used to promote the selective desilylation. This method enables the efficient synthesis of unsymmetric acetylenes with other silylated functional groups present. Further possibilities of the method were explored by synthesis of heterocycles.