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Biginelli-like reaction with dialkyl acetone-1,3-dicarboxylates: a remarkable case of steric control

✍ Scribed by Jan Sve˘tlík; Lucia Veizerová; Viktor Kettmann


Book ID
104095275
Publisher
Elsevier Science
Year
2008
Tongue
French
Weight
226 KB
Volume
49
Category
Article
ISSN
0040-4039

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✦ Synopsis


A Biginelli-type condensation is described using dialkyl acetone-1,3-dicarboxylates as active methylene compounds for the preparation of monastrol analogues. Unexpectedly, the reaction with salicylaldehyde formed two different products depending on the ester alkyl group. This product dichotomy was found to be caused by the steric effects exerted by the alcohol terminus of the ester group in the active methylene component. Previous controversial results as to the structure of the Biginelli product 3 are also discussed.