C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/58 (2006.01) C07F 9/38 (2006.01)
Patent
CA 2399974
The present invention relates to a novel process for making geminal bisphosphonates. The process provides for bisphosphorylation using phosphorus trihalide, phosphorous acid as a reactant/solvent, and a base as an acid acceptor/solvent. The present invention is directed to a process for making geminal bisphosphonates of the general formula (I), wherein Q is oxygen, -NR4-, sulfur, selenium, or a single bond; m+n is an integer from 0 to about 5, Z is a ring selected from the group consisting of pyridine, pyridazine, pyrimidine, and pyrazine; R1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, alkoxy, halogen, carboxylate, substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; each R2 is independently, hydrogen, or substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 4 carbon atoms; R3 is one or more substituents selected from the group consisting of hydrogen, substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, vitro, amido, amino, substituted amino, carboxylate, and combinations thereof; R4 is hydrogen, substituted alkyl (saturated or unsaturated) having from I to about 4 carbon atoms, or acyl.
La présente invention concerne un nouveau procédé de fabrication de bisphosphonates géminés. Ce procédé fait intervenir une bisphosphorylation au moyen de trihalogénure de phosphore, un acide phosphoreux comme réactif/solvant et une base comme accepteur/solvant acide. Cette invention concerne la fabrication de biphosphonates géminés représentés par la formule générale (I). Dans cette formule, Q est oxygène, -NR4-, soufre, sélénium, ou une liaison unique; m+n est un entier compris entre 0 et environ 5, Z est un noyau pris dans le groupe comprenant la pyridine, la pyridazine, la pyrimidine, et la pyrazine; R1 est hydrogène, amino substitué ou non substitué, amido, hydroxy, alkoxy, halogène, carboxylate, alkyle, (saturé ou insaturé) substitué ou non et comptant de 1 à 6 atomes de carbone, aryle substitué ou non, ou benzyle substitué ou non; chaque R2 est indépendamment hydrogène ou alkyle (saturé ou insaturé) substitué ou non, avec de 1 à 4 atomes de carbone environ; R3 est un ou plusieurs substituants pris dans le groupe comprenant hydrogène, alkyle (saturé ou insaturé) substitué ou non,comptant de 1 à environ 6 atomes de carbone, aryle substitué et non substitué, benzyle substitué et non substitué, hydroxy, halogène, carbonyle, alkoxy, nitro, amido, amino, amino substitué, carboxylate, seuls ou en combinaisons; R4 est hydrogène, alkyle (saturé ou insaturé) substitué, comptant de 1 à environ 4 atomes de carbone, ou acyle.
Billings Dennis Michael
Cazer Frederick Dana
Cramer William Douglas
Parry Gregory Eugene
Ledgley Law
The Procter & Gamble Company
Warner Chilcott Company Llc
LandOfFree
Process for making geminal bisphosphonates does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Process for making geminal bisphosphonates, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for making geminal bisphosphonates will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1933172