48074-47-1

Usage

InChI:InChI=1/C14H30O6P2/c1-10(2)17-21(15,18-11(3)4)14(9)22(16,19-12(5)6)20-13(7)8/h10-13H,9H2,1-8H3

Upstream product

• 1660-95-3 Tetraisopropyl methylenediphosphonate 
• 50-00-0 formaldehyd 
• 4410-92-8 N,N'-diethylmethanediamine 

Downstream Products

• 1192135-61-7 C₂₀H₃₇NO₇P₂ 
• 1192135-63-9 C₂₄H₄₄N₂O₇P₂ 
• 1192135-70-8 C₂₄H₄₄N₂O₆P₂ 

Relevant academic research and scientific papers

Polyethylenimine-Bisphosphonate-Cyclodextrin Ternary Conjugates: Supramolecular Systems for the Delivery of Antineoplastic Drugs

Bisphosphonates (BPs) are bone-binding molecules that provide targeting capabilities to bone cancer cells when conjugated with drug-carrying polymers. This work reports the design, synthesis, and biological evaluation of polyethyleneimine-BP-cyclodextrin (PEI-BP-CD) ternary conjugates with supramolecular capabilities for the loading of antineoplastic drugs. A straightforward, modular, and versatile strategy based on the click aza-Michael addition reaction of vinyl sulfones (VSs) allows the grafting of BPs targeting ligands and βCD carrier appendages to the PEI polymeric scaffold. The in vitro evaluation (cytotoxicity, cellular uptake, internalization routes, and subcellular distribution) for the ternary conjugates and their doxorubicin inclusion complexes in different bone-related cancer cell lines (MC3T3-E1 osteoblasts, MG-63 sarcoma cells, and MDA-MB-231 breast cancer cells) confirmed specificity, mitochondrial targeting, and overall capability to mediate a targeted drug transport to those cells. The in vivo evaluation using xenografts of MG-63 and MDA-MB-231 cells on mice also confirmed the targeting of the conjugates.

Synthesis of novel bisphosphonate polyamine conjugates and their affinity to hydroxyapatite

Bisphosphonates are negatively charged molecules, widely used as bone drugs since they have high affinity to bone surface. Polyamines are small organic bases that are positively charged under the physiological conditions and they participate in the regulation of important cellular functions. In this study, we report a general synthesis strategy for bisphosphonate-polyamine conjugates starting from ethenylidene bisphosphonates and N-Boc protected polyamines. Four novel conjugates were prepared and characterized with spectroscopic methods. The affinity of these novel compounds to hydroxyapatite was also determined by using 99mTc procedure. ARKAT-USA, Inc.

Antimicrobial agents and process for their manufacture

Disclosed are tetraalkyl enthenylidenebisphosphonates and a method for their manufacture. These compounds are suitable for use as antimicrobial agents in combating a number of pathogenic microorganisms, such as bacteria, yeasts, viruses, fungi and protozoa, when used together with a pharmaceutically-acceptable carrier. Also disclosed is a method for treating infectious diseases by administering a safe and effective amount of these tetraalkyl ethenylidenebisphosphonates.

Synthesis of Ethenylidenebis(phosphonic acid) and Its Tetraalkyl Esters

A new method for the preparation of tetraalkyl ethenylidenebis(phosphonates) has been developed.This two-step procedure involves the base-catalyzed reaction of a methylenebis(phosphonate) ester with paraformaldehyde followed by acid-catalyzed elimination of methanol.The effects of variations in the reaction conditions of the first step of this process are described.Ethenylidenebis(phosphonate) esters can be converted to the free acid by reaction with bromotrimethylsilane.