Method for preparing cyclopropyl boronic acid

The invention discloses a method for preparing cyclopropyl boronic acid. Cyclopropyl methanoic acid is adopted as a raw material and added into a solution obtained after n-butyllithium reacts with organic alkali at the low temperature, and then a boronizing reagent is added into the mixture; after b...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Hauptverfasser:	GUI WENWU, LENG YANGUO, GUI QIAN
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM CHEMISTRY METALLURGY ORGANIC CHEMISTRY
Online-Zugang:	Volltext bestellen
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The invention discloses a method for preparing cyclopropyl boronic acid. Cyclopropyl methanoic acid is adopted as a raw material and added into a solution obtained after n-butyllithium reacts with organic alkali at the low temperature, and then a boronizing reagent is added into the mixture; after boronation is finished, acid is added for quenching to obtain 1-carboxyl cyclopropyl boronic acid; the intermediate is added into high-boiling-point solvent and heated until the temperature is 80 DEG C-150 DEG C, after reaction deacidification, methylbenzene is added into the mixed solution for dehydration to form cyclopropyl boronic acid trimer, and the cyclopropyl boronic acid trimer is hydrolyzed to obtain the cyclopropyl boronic acid; the melting point of the obtained cyclopropyl boronic acid is 90 DEG C-95 DEG C, and the HNMR purity of the obtained cyclopropyl boronic acid is over 98%. The method is easy to operate and suitable for industrial scale-up production, and no highly toxic chemical is used in the whole process.