146432-41-9

Upstream product

• 5292-43-3 bromoacetic acid tert-butyl ester 
• 141-43-5 ethanolamine 
• 23147-58-2 glycolaldehyde dimer 
• 85916-13-8 tert-butyl iminodiacetate 

Downstream Products

• 1000991-93-4 C₃₄H₅₅N₃O₁₂ 
• 1000991-94-5 C₃₄H₅₇N₃O₁₀ 
• 1566605-69-3 1,1-bis(benzyloxycarbonylmethyl)-4-methoxycarbonylmethyl-7,7-bis(tert-butoxycarbonylmethyl)-1,4,7-triazaheptane 
• 1566605-70-6 1-benzyl-1-methoxycarbonylmethyl-4,4-bis(tert-butoxycarbonylmethyl)-1,4-diazabutane 
• 1566605-88-6 C₆₆H₁₁₁N₉O₂₁ 
• 1566605-87-5 C₄₈H₈₃N₇O₁₇ 
• 1566605-86-4 C₄₇H₈₁N₇O₁₇ 
• 1566605-85-3 C₆₂H₉₅N₇O₁₇ 
• 1566605-79-5 C₄₄H₆₇N₅O₁₄ 
• 1566605-75-1 C₅₁H₈₉N₇O₁₈ 
• 1163255-14-8 4-benzyloxycarbonylmethyl-1,1,7,7-tetra(carboxymethyl)-1,4,7-triazaheptane 
• 178552-82-4 4-benzyloxycarbonylmethyl-1,1,7,7-tetra(tertbutyloxycarbonylmethyl)-1,4,7-triazaheptane 
• 174267-71-1 3,9-Bis(tert-butoxycarbonylmethyl)-6-carboxymethyl-3,6,9-triazaundecanedioic acid-di-tert-butyl ester 
• 1362022-22-7 C₃₈H₆₄N₄O₁₁ 

Relevant academic research and scientific papers

An unusual tandem cyclization-Stevens rearrangement mediated by Ph3P/DEAD or Bu3P/ADDP

Alcohols 1 and 10c when treated with Ph3P/DEAD or Bu3P/ADDP yield products resulting from intramolecular cyclization to form five- and six-membered, cyclic quaternary ammonium salts (respectively) which undergo a Stevens rearrangement in the same pot.

Comparing hypoxia-targeting potential of 99mTc(CO) 3-labeled 2-nitro and 4-nitroimidazole

Non-invasive determination of hypoxia is an important problem in clinical nuclear medicine. Although 18F-fluoromisonidazole is used clinically for hypoxia determination, the short half-life t1/2 = 109.77 min), high cost and less availability of cyclotrone-produced 18F make 99mTc (t1/2 = 6 h)-based agents more desirable. With this aim, 99mTc(CO)3-labeled iminodiacetic acid derivatives of 2- and 4-nitroimidazole are investigated for their ability to target hypoxic tumors. A bifunctional chelating agent, N, N-bis[(tert-butoxycarbonyl)methyl]-2- bromoethylamine, was synthesized in the first step, which was then conjugated to the nitroimidazoles in the second step. The tert-butyl ester derivatives formed were hydrolyzed to obtain the iminodiacetic acid derivatives of corresponding nitroimidazoles. The radiolabeling of the iminodiacetic acid derivatives with [""1Tc(CO)3(H2O)3I+ core was carried out following a reported protocol. Biodistribution of the prepared complexes was carried out in Swiss mice bearing fibrosarcoma tumor. The 2-nitroimidazole complex showed a steady retention in activity ( - 1.5% injected dose per gram [%ID/g]) in tumor throughout the period of study (3 h) indicating that it may be localized in the hypoxic cells. The 4-nitroimidazole counterpart, however, showed an initial uptake of ～4.6%ID/g at 30 min post injection, which was then observed to wash out rapidly. Copyright

Evaluation of 99mTc(CO)3 complex of 2-methyl-5-nitroimidazole as an agent for targeting tumor hypoxia

An iminodiacetic acid (IDA) derivative of 2-methyl-5-nitroimidazole was synthesized as a carrier molecule for radiolabeling with the gamma emitting radioisotope, 99mTc, for imaging hypoxic regions of tumors. The ligand was synthesized in excellent yield and labeled using freshly prepared [99mTc(CO)3(H2O)3]+ intermediate. A complexation yield of over 95% could be achieved under mild conditions using a ligand concentration of 1 mg/mL [～3 × 10-3 M]. The complex was characterized by HPLC and its stability in human serum was studied. Biodistribution studies performed in Swiss mice bearing fibrosarcoma tumor showed maximum accumulation in the tumor to the extent of ～0.52 %ID/g at 30 min post-injection (pi). The major clearance of the complex was through the hepatobiliary route. The complex showed tumor/muscle ratio of 1.75 at 30 min pi, which significantly increased to 17 at 180 min pi. However, the tumor/blood ratio was below one throughout the period of study, which could be due to slow clearance of the complex from blood.

Gd-functionalised Au nanoparticles as targeted contrast agents in MRI: Relaxivity enhancement by polyelectrolyte coating

Monolayer-protected, Gd3+-functionalised gold nanoparticles with enhanced spin-lattice relaxivity (r1) were prepared; adsorption of polyelectrolytes on these materials further increased r1 and ligand exchange with a biotin-derivatised disulfide led to a prototype avidin-targeted contrast agent.

Selective protein purification by PEG-IDA-functionalized iron oxide nanoparticles

We developed a new heterobifunctional polyethylene glycol ligand for iron oxide nanoparticles with a group for covalent surface attachment and for chelating metal ions. After introduction of nickel ions, His-tagged fluorescent proteins were magnetically purified from a cell lysate. A high purity product and efficient magnetic separation were observed.

Radioactivity-synchronized fluorescence enhancement using a radionuclide fluorescence-quenched dye

(Chemical Equation Presented) We demonstrate the first evidence of radioactivity-synchronized fluorescence quenching of a near-infrared light-emitting dye by a radionuclide, 64Cu, and subsequent fluorescence enhancement upon 64Cu decay to the daughter isotopes 64Ni and 64Zn. The dynamic switch from high radioactivity and low fluorescence to low radioactivity and high fluorescence is potentially useful for developing complementary multimodal imaging and detection platforms for chemical, environmental, and biomedical applications as well as for unraveling the mechanisms of metal-induced dynamic fluorescence changes.

Discrete nanomolecular polyhedral borane scaffold supporting multiple gadolinium(III) complexes as a high performance MRI contrast agent

An icosahedral closo-B122- scaffold supports 12 copies of Gd3+-chelate held in close proximity with each other by suitable linkers which employ azide-alkyne click chemistry. This design is the first member of a new class of polyfunctional MRI contrast agents carrying a high payload of Gd3+-chelate in a sterically constrained configuration. The resulting contrast agent shows higher relaxivity values at high magnetic fields. MRI contrast agents currently in use are not as effective in this regard, presumably due to a lack of steric constraint of gadolinium centers and lower water exchange rates. In vivo MRI studies in mice show excellent contrast enhancement even at one-seventh of the safe clinical dose (0.04 mmol Gd/kg) for up to a 1 h exposure.

BIHETEROCYCLIC COMPOUND

The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter wherein R1-L- is R1—OC(O)—, or the like, R1 is hydrogen atom, optionally-substituted C1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R3 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like, the part of X, Y, and Z is X═Y—Z, X—Y═Z, or X—Y—Z, X is nitrogen atom, NR4 (R4 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.

METAL CHELATORS FOR IMAGING, THERAPEUTICS, AND BIOANALYSIS

A variety of compounds are provided capable of chelating a metal, in particular a lanthanide such as Eu(III) and Tb(III). Luminescent complexes of the compound and a metal ion are also provided, in particular luminescent metal complexes are provided containing a lanthanide such as Eu(III) or Tb(III) and a compound described herein. In some aspects, the luminescent complexes are capable of exhibiting bright emissions with high quantum yields. Methods of making the compound are provided. Methods of using the compounds and luminescent complexes are also provided, for example for imaging and therapeutic applications.

Dual modal imaging agents based on chromophore-bearing DTPA analogues

Two new DTPA analogues, centrally (L1) and terminally (L2) functionalised with a 1,8-naphthalimide chromophore, have been successfully prepared and fully characterized. Their Gd(iii) complexes have also been prepared and evaluated for their ability to act as dual modal contrast agents (MRI/OI). The highly reproducible R1 relaxivity of L1 (8.10 ± 0.21 mM-1 s-1, 25 °C and 30 MHz) is markedly higher than other DTPA based contrast agents. The Gd(iii) complexes of both L1 and L2 have been evaluated as luminescence probes; the ligand based fluorescence is not quenched upon complexation.