Process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-biphosphonic acid
AssigneeEos Eczacibasi Ozgun Kimyasal Urunler Sanayi Ve Ticaret A.S.
InventorsKadir Dabak, A. Evren Ozarslan, Filiz Sahbaz, Tuncer Aslan
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Abstract
This invention is related with the preparation of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof. The reaction of 4-aminobutyric acid with phosphorous acid and phosphorus trichloride in the presence of aralkyl or alkyl ethoxylates or triglycerides such as plant or animal oils or their derivatives; and recovering of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof are described. The main feature of the invention is in the use of the above defined non-ionic emulgators in the phosphonylation reaction.
Claims15
A process for preparation of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof, comprising the steps of:
- (a) reacting 4-aminobutyric acid with phosphorous acid and phosphorous trichloride in the presence of aralkyl ethoxylates or alkyl ethoxylates, having the formula of R—X—O—(CH2CH2O)n—H, or in the presence of triglycerides selected from the group consisting of plant oils or animal oils, having the formula of (RCO2CH2)2CHCOOR, wherein R represents branched or non-branched alkyl groups having 1 to 20 carbon atoms or alkenyl groups having 2 to 20 carbon atoms, n is a number between 1 and 30 and X is a variable which represents phenyl or naphthyl or —CH2— when R is an alkenyl group and which represents phenyl or naphthyl when R is an alkyl group;
- (b) recovering said 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof by an hydrolysis reaction of mono-, di-, tri- or poly phosphorous esters of 4-aminobutyric acid.
Dependencies are inferred from the claim text.