玛巴洛沙韦类似物:三环构建策略和应用

文摘   2024-09-02 07:00   天津  
文献题目
Hydroformylation and Late-Stage Diversification on Densely Functionalized Cores of Influenza Endonuclease Inhibitors

文献摘要
Our approaches toward this goal encompass (i) the development of a modular, diastereoselective route to the tricyclic cores and (ii) the use of advanced intermediates for late-stage diversification. Key to realizing both strategies is the development of an efficient, functional group-tolerant, chemoselective hydroformylation step that can be executed in the presence of the metal binding motif common to this inhibitor family. 


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逆合成思路

三环构建策略
制备化合物6

化合物6的关环研究






策略应用


(i) 30 (1.0 equiv), Comin’s reagent (2.0 equiv), 2-tertbutyl-1,1,3,3-tetramethylguanidine (2.0 equiv), THF, RT, 1 h. (ii) 34 (1.0 equiv), p-tolylboronic acid (2.5 equiv), Xantphos Pd G3 (0.10 equiv), Cs2CO3 (3.0 equiv), dioxane/H2O (5:1), 90 °C, 16 h. (iii) 34 (1.0 equiv), pyridine boronic acid (3.0 equiv), PPh3 Pd G2 (0.10 equiv), Cs2CO3 (3.0 equiv), dioxane/H2O (2.5:1), 90 °C, 4 h.

参考文献
https://doi.org/10.1021/acs.oprd.4c00277

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