Combining the use of solid-supported transition metal catalysis with microwave irradiation in solution-phase parallel library synthesis

被引：24

作者：

Organ, Michael G. ^{[1
]}

Mayer, Stanislas ^{[1
]}

Lepifre, Franck ^{[1
]}

N'Zemba, Blaise ^{[1
]}

Khatri, Jayantilal ^{[1
]}

机构：

[1] York Univ, Dept Chem, Toronto, ON M3J 1P3, Canada

来源：

MOLECULAR DIVERSITY | 2003年 / 7卷 / 2-4期

基金：

加拿大自然科学与工程研究理事会;

关键词：

acetylcholine receptor agonist and antagonist; COX II inhibitors; factor Xa inhibitors; microwave irradiation; parallel synthesis; Pd catalysis; solid-supported catalyst;

D O I：

10.1023/B:MODI.0000006826.91512.83

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Microwave heating methods have been combined with the use of solid-supported catalysts to produce small solution-phase libraries of medicinally-relevant compounds. Palladium supported on charcoal (Pd/C) has been used to produce libraries of pyrazole compounds for screening in COX II studies via Suzuki cross coupling reactions, while the same catalyst has been used also to produce styryl-based nAChR compounds using analogous chemistry. Although the reaction substrates are very different ( aryl vs. vinyl), this catalyst system provided consistently good and reliable results. The use of a polystyrene-supported Ru catalyst for ring-closing metathesis (RCM) reactions was also evaluated to prepare benzolactam structures for evaluation as factor Xa inhibitors.

引用

页码：211 / 227

页数：17

共 34 条

[1] A recyclable 'boomerang' polymer-supported ruthenium catalyst for olefin metathesis [J].