First- and Second-Generation
Practical Syntheses of
Chroman-4-one Derivative: A Key Intermediate for the Preparation of
SERT/5-HT<sub>1A</sub> Dual Inhibitors
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Abstract
Two approaches to large-scale synthesis of the key intermediate <b>9</b>, a precursor of novel dual inhibitors of SERT/5-HT<sub>1A</sub> receptor, are described. These two approaches each feature a mild
and efficient method for construction of the chroman-4-one scaffold,
which can be used with substrates containing base-sensitive functionalities
and enable synthesis on kilogram scale without chromatographic purification.
The first-generation synthesis enables quick delivery of a kilogram
quantity of the key intermediate <b>9</b> with only one slurry
purification step. On the other hand, the highly practical second-generation
synthesis is suitable for the multikilogram campaign