which of the following ketones cannot be prepared using acetoacetic ester synthesis? course hero

by Prof. Karlie Rath 8 min read

What is acetoacetic ester synthesis?

The acetoacetic ester synthesis is a useful synthetic tool for preparing ketones having one or two alkyl groups on the ɑ position: At first, this may look confusing since there is a whole ester group being lost in the course of the reaction.

What happens to the ester in the first part of the reaction?

In the first part, the ester is hydrolyzed to a carboxylic acid which then loses carbon dioxide through a nicely arranged six-membered transaction state:

What is the purpose of the ester group?

The only purpose of the ester group is to make the ɑ hydrogen between the ketones more acidic. Remember, dicarbonyl compounds are about twice more acidic compared to their analogs with only one electron-withdrawing group:

Can cyclohexanone be deprotonated?

The answer is yes, we can do that, however, having a more acidic ɑ hydrogen allows for using a weaker base and therefore, carrying out the reaction in milder conditions. For example, alkylation of cyclohexanone requires using LDA, while acetoacetic ester can be deprotonated by sodium ethoxide:

Can hydroxide base hydrolyze carboxylic salt?

A hydroxide base, on the other hand, may hydrolyze the ester to a carboxylic salt before deprotonating the ɑ carbon: Using an alkoxide of a different alkyl group wouldn’t matter in a long run since the ester group is cleaved off at the end anyway:

Does alkoxide have the same alkyl group as keto?

The alkoxide ion should have the same alkyl group as the ester of the starting β-keto ester. For example, to deprotonate the ethyl acetoacetic ester, an ethoxide salt must be used. If a methoxide or a hydroxide is used, a problem of transesterification occurs: A hydroxide base, on the other hand, may hydrolyze the ester to a carboxylic salt ...