Search

The title reaction can be also applied to the synthesis of compound (IX), a useful precursor for the preparation of befloxatone, which is a reversible and selective monoamine oxidase A inhibitor.

A novel chiral difluoroallylboronate (I) is applied to the reaction with various aromatic and aliphatic aldehydes affording α-gem-difluorohomoallyl alcohols.

Still—Gennari olefination of substrates (II) affords exclusively the (Z)-isomers (IV) which are transformed to the required pyrones (VI) (important building blocks of natural products) via (Z)-alcohols (V).

The reaction of aldehydes and ketones with primary and secondary amines under conditions A) and B) affords secondary and tertiary amine products in excellent yields.