Microwave-assisted acylation of 7-amino-5-aryl-6-cyanopyrido[2,3-d]pyrimidines

A microwave-assisted method is described for monoacylating 7-amino-5-aryl-6-cyanopyrido[2,3-d]pyrimidines using excess acid chlorides in pyridine. A diacylated intermediate is effectively deacylated to the product amide by a macroporous-Tris resin. A small library of 17 amides was prepared to valida...

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Bibliographic Details
Published inMolecular diversity Vol. 7; no. 2-4; pp. 247 - 252
Main Authors Nicewonger, Robb, Fowke, April, Nguyen, Kathy, Ditto, Lori, Caserta, Justin, Harris, Michele, Baldino, Carmen M
Format Journal Article
LanguageEnglish
Published Netherlands Springer Nature B.V 2003
Subjects
Acids - chemistry
Acylation
Amides
Chlorides - chemistry
Chromatography, High Pressure Liquid
Heating
Microwave heating
Microwaves
Models, Chemical
Peptides - chemistry
Pyridines - chemistry
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Ultraviolet Rays
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Summary:A microwave-assisted method is described for monoacylating 7-amino-5-aryl-6-cyanopyrido[2,3-d]pyrimidines using excess acid chlorides in pyridine. A diacylated intermediate is effectively deacylated to the product amide by a macroporous-Tris resin. A small library of 17 amides was prepared to validate the method. The integration of commercial microwave technology into the ArQule chemistry platform is also discussed.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1381-1991
1573-501X
DOI:10.1023/B:MODI.0000006907.21070.11