133918-47-5

Upstream product

• 15205-57-9 tribenzyl phosphite 
• 166049-87-2 dibenzyl (chloromethyl)phosphonate 
• 1984-15-2 Methylenediphosphonic acid 
• 29134-54-1 tris(benzyloxy)methane 
• 253682-73-4 dibenzyl (bromomethyl)phosphonate 
• 538-37-4 dibenzyl phosphochloridate 
• 19236-58-9 dibenzyl methylphosphonate 
• 17176-77-1 Dibenzyl phosphite 
• 114790-35-1 dibenzyl hydroxymethylphosphonate 
• 1499-29-2 P,P'-methanediyl-bis-phosphonic acid tetrachloride 
• 100-51-6 benzyl alcohol 
• 16001-93-7 tetramethyl methylenediphosphonate 
• 100-44-7 benzyl chloride 

Downstream Products

• 183383-55-3 tetrabenzyl 2-t-butoxycarbonylethane-1,1-diphosphonate 
• 263552-46-1 (2R,3R), 3-benzyloxycarbonylamino-2-[4-methoxybenzylsulfanyl]-5-[dibenzyloxyphosphoryl]-pent-4-enoic acid tertiobutyl ester 
• 346722-77-8 ethyl 3,3-bis(dibenzyloxyphosphoryl)propanoate 
• 877760-65-1 tetrabenzyl [3-azido-1,2-O-isopropylidene-3,5,6-trideoxy-α-L-glucofuranos-6,6'-diyl]biphosphonate 
• 1421705-33-0 (1’S)-dibenzyl C-(2,3,5,6-tetra-O-benzyl-α-D-galactofuranosyl)-1'-acetoxymethanephosphonate 
• 1421705-12-5 (E)-1,1'-dideoxy-1'-(dibenzylphosphinyl)-2,3,4,5,6-penta-O-benzyl-D-galacto-hept-1'-enitol 
• 1417995-18-6 C₂₆H₂₄N₃O₅P 
• 1417995-22-2 C₁₉H₂₁O₃P 
• 1417995-23-3 C₁₉H₂₁O₃P 
• 346722-74-5 4,4-Bis-(bis-benzyloxy-phosphoryl)-butyric acid (8R,9S,13S,14S,17S)-3-benzyloxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl ester 
• 346722-75-6 3,3-Bis-(bis-benzyloxy-phosphoryl)-propionic acid (8R,9S,13S,14S,17S)-3-benzyloxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl ester 
• 346722-73-4 4,4-Bis-(bis-benzyloxy-phosphoryl)-butyric acid (3S,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl ester 
• 346722-76-7 3,3-Bis-(bis-benzyloxy-phosphoryl)-propionic acid (3S,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-17-oxo-hexadecahydro-cyclopenta[a]phenanthren-3-yl ester 

Relevant academic research and scientific papers

Rh(III)-catalyzed, 1,2,3-triazole-assisted directed C–H coupling with diazo diphosphonates

A mild and efficient procedure was developed for the [Cp?Rh(III)]-catalyzed, 1,2,3-triazole directed C–H coupling with diazomethylene-diphosphonates. This protocol provided a step- and atom-economical protocol for C–C bond formation and led to structurally diverse 2-(1,2,3-triazol-2-yl)benzyl diphosphonates in good to excellent yields.

Selenophosphonates as building blocks for the preparation of bis-methylene analogs of triphosphates

A new route to bis-methylene analogs of triphosphate esters involving carbanion chemistry is described. Lithiated methaneselenophosphonate anion is condensed several times with chlorophosphites and phosphoramidous chlorides prior to esterification/transesterification and selenation or oxidation.

Bisphosphonate prodrugs: A new synthetic strategy to tetraacyloxymethyl esters of methylenebisphosphonates

A concise and simple method to prepare Cl2C[P(O)(OCH2O2CCMe3)2]2 starting from H2C[P(O)(OMe)2]2 with high selectivity and reasonable yield is developed.

COMPOSITIONS AND METHODS OF MODULATING THE IMMUNE RESPONSE BY ACTIVATING ALPHA PROTEIN KINASE 1

The disclosure provides compositions and methods related to activating alpha-kinase 1 (ALPK1) for modulating an immune response and treating or preventing cancer, infection, inflammation and related diseases and disorders as well as potentiating an immune response to a target antigen. The disclosure also provides heterocyclic compounds of formula (I) as agonists of alpha protein kinase 1 (ALPK1) and their use in activating ALPK1, modulating an immune response and treating diseases such as cancer, wherein A1, A2, L1, L2, L3, Z1, Z2, W1, W2, R1, R2, R3, R4, R5, R6 and R7 are defined herein.

PET bone imaging agent precursor and synthesis method thereof

The invention discloses a PET bone imaging agent precursor, wherein a linking agent tripolyethanol is introduced between a macrocyclic polyamine ligand and a targeting carrier diphosphonic acid, and the diphosphonic acid bone-seeking group with targeting effect can form the macrocyclic polyamine cooperation group of a stable chelate with a plurality of metal nuclides so as to form a bone imaging agent. According to the present invention, the synthesized precursor compound contains the bone-seeking group (diphosphonic acid) and the cooperation group (DOTA), and the two functional groups are linked by PFG3, such that the precursor compound has remarkable structural characteristics; the precursor compound has strong bone-seeking property, and can form a complex (marker) with kinetic and thermodynamic stability with metal nuclides; the marker formed by marking the precursor with different metal nuclides can be used as a bone imaging agent (marked with Cu, Ga and other positron emission metal nuclides) with powerful functions, and can further be used as an ideal bone tumor treatment drug (marked with In, Y, Zr, Sm and other radioactive treatment metal nuclides).

PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS

The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.

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.

An osteoclast-targeting agent for imaging and therapy of bone metastasis

A hybrid compound (DO3A-BP) featuring a radiometal bifunctional chelator (1,4,7,10-tetraazacyclotetradecane-N,N′,N″,N?-tetraac etic acid, DOTA) and an osteoclast-targeting moiety (bisphosphonate) was designed and synthesized. The 111In-labeled complex of DO3A-BP showed significantly elevated uptake in osteoclasts compared to the undifferentiated adherent bone marrow derived cells. Biodistribution studies revealed a favorable tissue distribution profile in normal mice with high bone uptake and long retention, and low or negligible accumulation in non-target organs.

ORALLY AVAILABLE SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONISTS AND ANTAGONISTS

The present invention relates to S1P analogs that have activity as S1Preceptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.

Synthesis of new potential chelating agents: Catechol-bisphosphonate conjugates for metal intoxication therapy

In a quest for better chelating therapy drugs for the treatment of intoxication by Fe, Al, or actinides, three new series of bisphosphonates conjugated with catechol were synthesized.