59611-59-5

Upstream product

• 762-04-9 Diethyl phosphonate 
• 122-51-0 orthoformic acid triethyl ester 
• 103-67-3 benzyl-methyl-amine 
• 762-04-9 phosphonic acid diethyl ester 
• 17105-71-4 N-methyl-N-benzylformamide 
• 122-52-1 triethyl phosphite 

Relevant academic research and scientific papers

Microwave-assisted synthesis of (aminomethylene)bisphosphine oxides and (aminomethylene)bisphosphonates by a three-component condensation

A practical method was elaborated for the synthesis of (aminomethylene)bisphosphine oxides comprising the catalyst- and solventfree microwave-assisted three-component condensation of primary amines, triethyl orthoformate and two equivalents of diphenylpho

Synthesis of N-methyl alkylaminomethane-1,1-diphosphonic acids and evaluation of their complex-formation abilities towards copper(II)

A series of N-methyl alkylaminomethane-1,1-diphosphonic acids (3a-g) with a common tertiary nitrogen atom (CH3-N-R) bearing linear or branched alkyl, cycloheptyl or phenylalkyl R substituents was synthesized in the reaction of diethylphosphonat

METAL COMPLEX COMPOUND, CANCER THERAPEUTIC COMPOSITION COMPRISING THE METAL COMPLEX COMPOUND AS ACTIVE INGREDIENT, AND INTERMEDIATE FOR PRODUCTION OF THE METAL COMPLEX COMPOUND

A metal complex compound which exhibits a high degree of adsorption to bone or inhibition of cell growth, and is highly effective for therapy of a cancer metastasized to bone and therapy of the primary carcinoma thereof; a therapeutic agent composition for a cancer containing as an active ingredient the metal complex compound or a physiologically acceptable salt thereof; and an intermediate for the metal complex compound are provided. More concretely, a metal complex compound represented by the following General Formula (1): (wherein R1 independently represents C1-C10 alkyl which may be branched or have a substituent; or a C3-C30 cyclic group which may have a substituent; and X represents CHR2, an oxygen atom or NR5); a therapeutic agent composition for a cancer containing it as an active ingredient; and an intermediate for the metal complex compound are provided.

Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis

Osteomyelitis is a difficult to treat bacterial infection of the bone. Delivering antibacterial agents to the bone may overcome the difficulties in treating this illness by effectively concentrating the antibiotic at the site of infection and by limiting the toxicity that may result from systemic exposure to the large doses conventionally used. Using bisphosphonates as osteophilic functional groups, different forms of fluoroquinolone esters were synthesized and evaluated for their ability to bind bone and to release the parent antibacterial agent. Bisphosphonated glycolamide fluoroquinolone esters were found to present a profile consistent with effective and rapid bone binding and efficient release of the active drug moiety. They were assessed for their ability to prevent bone infection in vivo and were found to be effective when the free fluoroquinolones were not.

Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections

The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.

PI-3 KINASE INHIBITOR PRODRUGS

The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.

ORGANISCHE PHOSPHORVERBINDUNGEN 75. Herstellung und Eigenschaften von Aminomethylendiphosphinaten und -diphosphonaten, RR1NCH2(OR3>2 und Derivaten

Substituted aminomethylene-bis(phosphinates) are obtained in good yield by the interaction of substituted aminomethylenedichlorides with phosphonites or from the three component reaction consisting of a primary amine, orthoformates and the half-esters of phosphonous acids. 3-Methylpyridyl-2-aminomethylene-bis(O-ethyl-methylphosphinate) hydrolizes easily in water to give the corresponding acid in which neither of the nitrogen atoms is protonated, .Amino- and alkylamino-methylene-bis(phosphonates) are obtained, in high yield, by the hydrogenolytic debenzylation of the corresponding benzyl-derivatives, using Pd/C as a catalyst.Aminomethylene-bis(phosphonate), H2NCH2 (7) is a water-clear liquid which can be molecularly distilled, b.p. 125-127 deg/0.1 Torr., 31P +20.28 ppm, JPCH 20.5 Hz.On prolonged standing at 20 deg C it forms slowly a half-ester. 7 gives the typical reactions of a primary amine.Thus on treatment with dimethylformamid-dimethylacetal it yields a formamidine 10, with isocyanates it forms urea derivatives e.g. 11 and 12, and with aldehydes Schiff's bases are produced e.g. 13 to 18.The latter can be hydrogenated using Pt/C as catalyst to give monosubstituted aminomethylenediphosphonates e.g. 23 and 24.However on hydrogenation of 18 over Pt/C 7 was obtained.Thus 2-pyrrylmethyl represents a new, with H2/Pt/C, cleavageable group when bound to nitrogen.Acylation of 7 yields the corresponding acyl-derivatives, e.g. 19 and 20, and interaction with cyanamide produces guanidinomethylene-diphosphonate 21.