Gamma-Aminobutyric Acid → Alendronic Acid

Reaktionsgleichung

[P:1]([OH:4])([OH:3])[OH:2].[NH2:5][CH2:6][CH2:7][CH2:8][C:9]([OH:11])=O.P(Cl)(Cl)Cl>>[CH2:7]([CH2:6][NH2:5])[CH2:8][C:9]([P:1]([OH:4])([OH:3])=[O:2])([P:1]([OH:4])([OH:3])=[O:2])[OH:11]

Komponenten

Edukt 3

HCID 119Gamma-Aminobutyric Acid

HCID 24387Phosphorus trichloride

HCID 107909Phosphorous acid

Produkt 1

HCID 2088Alendronic Acid

Reaktionsbedingungen

Temperatur: 70 °C

Versuchsvorschrift

The mixture of 5 eq. phosphorous acid, 4-aminobutyric acid and morpholine. HCl is melted together until uniform solution is formed. The reaction mixture is cooled to about 70° C. and 2 eq. of PCl3 are carefully added. The mixture is heated for about 5.5 hours before the reaction mixture is hydrolyzed in aqueous acid at about 80° C. and alendronate is isolated from an ethanolic solution.

Aufarbeitung

customis formed
temperatureThe mixture is heated for about 5.5 hours before the reaction mixture
customis hydrolyzed in aqueous acid at about 80° C.

Quellen und Nachweise

ORD-Eintrag: ord-b3a0f7fd2bd7403f9357ce99aee0cb71
Quelldatensatz: uspto-grants-2003_05
DOI: 10.6084/m9.figshare.5104873.v1
Patentnummer: US06562974B2

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