Pd-catalyzed arylation of linear and angular spirodiamine salts under aerobic conditions

被引：8
作者：
Reilly, Sean W. [1 ]
Bryan, Nikaela W. [2 ]
Mach, Robert H. [1 ]
机构：
[1] Univ Penn, Perelman Sch Med, Dept Radiol, 231 S 34th St, Philadelphia, PA 19104 USA
[2] Univ Penn, Dept Syst Pharmacol & Translat Therapeut, 421 Curie Blvd, Philadelphia, PA 19104 USA
来源：
TETRAHEDRON LETTERS | 2017年 / 58卷 / 05期
基金：
美国国家卫生研究院;
关键词：
Pd cross-coupling; C-N cross-coupling; Arylation; Spirodiamine; RuPhos; CROSS-COUPLING REACTIONS; IIB-IIIA ANTAGONISTS; MEDICINAL CHEMISTRY; GHRELIN RECEPTOR; BUILDING-BLOCKS; ARYL HALIDES; INVERSE AGONISTS; DRUG DISCOVERY; POTENT; DESIGN;
D O I：
10.1016/j.tetlet.2016.12.063
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Application of Buchwald-Hartwig catalysis for development of biologically relevant arylspirodiamine compounds is reported. This synthetic methodology requires no inert atmosphere and affords yields up to 93% in just 20 min. Linear and sterically hindered angular spirodiamines in salt and free-base form are coupled with electron-rich and-withdrawing aryl chlorides, demonstrating a broad scope and applicability of this protocol. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码：466 / 469
页数：4
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