Shortened synthesis using paraformaldehyde or trioxane

The present disclosure relates to a process for the preparation of a compound of formula (I): wherein R is hydrogen, a formyl group, a straight, branched or cyclic C1-C6 alkylcarbonyl group or a phenylcarbonyl group, or a salt thereof, characterized by the steps of reacting a compound of formula (I...

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Bibliographische Detailangaben
Hauptverfasser: CORNELIA FUCHS, DEAN JOHNSON, RALF KANZLER, SETH C. ENNIS
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:The present disclosure relates to a process for the preparation of a compound of formula (I): wherein R is hydrogen, a formyl group, a straight, branched or cyclic C1-C6 alkylcarbonyl group or a phenylcarbonyl group, or a salt thereof, characterized by the steps of reacting a compound of formula (II): with a mixture of Grignard initiator and Mg in a solvent to form a Grignard reagent, reacting the Grignard reagent with paraformaldehyde or trioxane to obtain a compound of formula (III): and then further reacting the compound of formula (III) in a known manner to obtain a compound of formula (I) and optionally salt formation.