通过选择性金属化和亚砜/镁交换实现 7-氮吲哚骨架的全功能化。
Full functionalization of the 7-azaindole scaffold by selective metalation and sulfoxide/magnesium exchange.
机构信息
Department Chemie, Ludwig-Maximilians-Universität München, Butenandtstrasse 5-13, 81377 München (Germany).
出版信息
Angew Chem Int Ed Engl. 2013 Sep 16;52(38):10093-6. doi: 10.1002/anie.201303490. Epub 2013 Jul 29.
PMID:23897626
Abstract
Filling positions: 7-Azaindoles are important targets in the pharmaceutical industry. All five carbon positions of the azaindole ring system can be functionalized in a predictable manner starting from the appropriately substituted azaindole 1 by directed metalation and halogen/magnesium and sulfoxide/magnesium exchange. The products are fully substituted azaindoles of type 2.
摘要
填充职位
7-氮杂吲哚是制药行业的重要目标。从适当取代的氮杂吲哚 1 出发，通过定向金属化和卤素/镁和亚砜/镁交换，可以以可预测的方式对氮杂吲哚环系统的所有五个碳位置进行官能化。产物是完全取代的 2 型氮杂吲哚。
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