当前位置: X-MOL 学术Angew. Chem. Int. Ed. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Concise Synthesis of Tunicamycin V and Discovery of a Cytostatic DPAGT1 Inhibitor
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-05-20 , DOI: 10.1002/anie.202203225
Katsuhiko Mitachi 1 , David Mingle 1 , Wendy Effah 2 , Antonio Sánchez-Ruiz 3 , Kirk E Hevener 1 , Ramesh Narayanan 2 , William M Clemons 4 , Francisco Sarabia 5 , Michio Kurosu 1
Affiliation  

A Büchner–Curtius–Schlotterbeck-type reaction enabled the total synthesis of tunicamycin V (TN-V), a nonselective phosphotransferase inhibitor, in just 15 steps from D-galactal in 21 % overall yield. The short and high-yielding synthetic route was also adapted for the synthesis of analogues, thus leading to the discovery of a novel cytostatic tunicamycin analogue, TN-TMPA, with high DPAGT1 selectivity.

中文翻译:

衣霉素 V 的简明合成和细胞抑制 DPAGT1 抑制剂的发现

Büchner-Curtius-Schlotterbeck 型反应只需 15 个步骤即可从 D-半乳糖全合成衣霉素 V (TN-V)(一种非选择性磷酸转移酶抑制剂),总产率为 21%。短而高产的合成路线也适​​用于类似物的合成,从而发现了一种具有高 DPAGT1 选择性的新型细胞抑制衣霉素类似物 TN-TMPA。
更新日期:2022-05-20
down
wechat
bug