Large scale Biginelli reaction via water-based biphasic media: a green chemistry strategy

Rapid reactions with excellent yield and high atom economy are described. An important stage in process development is kilo scale preparation of the target compound. For this reason, a procedure involving water-based biphasic reaction media has been developed for conducting some exothermic reactions...

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Bibliographic Details
Published inTetrahedron letters Vol. 46; no. 11; pp. 1901 - 1903
Main Authors Bose, Ajay K., Manhas, Maghar S., Pednekar, Suhas, Ganguly, Subhendu N., Dang, Hoang, He, William, Mandadi, Arun
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 14.03.2005
Elsevier
Subjects
Biginelli reaction
Biphasic media
Chemistry
Chemistry, Organic
Dihydropyrimidinones
p-TSA as catalyst
Physical Sciences
Science & Technology
p-TSA as catalyst
Biphasic media
Biginelli reaction
Dihydropyrimidinones
dihydropyrimidinones
biphasic media
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Summary:Rapid reactions with excellent yield and high atom economy are described. An important stage in process development is kilo scale preparation of the target compound. For this reason, a procedure involving water-based biphasic reaction media has been developed for conducting some exothermic reactions on a large scale. This protocol is illustrated by the energy-efficient and rapid preparation of dihydropyrimidinones by a solvent-free, green chemistry procedure applied to the Biginelli reaction using p-toluenesulfonic acid as catalyst.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2005.01.087