53733-98-5

Upstream product

• 501-53-1 benzyl chloroformate 
• 60-32-2 6-aminohexanoic acid 
• 6066-82-6 1-hydroxy-pyrrolidine-2,5-dione 
• 1947-00-8 6-(benzyloxycarbonylamino)hexanoic acid 
• 541-41-3 chloroformic acid ethyl ester 
• 5105-78-2 4-(benzyloxycarbonylamino)butyric acid 
• 75513-55-2 N-hydroxysuccinimido diphenyl phosphate 
• 74124-79-1 di(succinimido) carbonate 

Downstream Products

• 56403-09-9 1,8-diazacyclotetradecane-2,9-dione 
• 25580-88-5 methyl 13-benzyloxycarbonylamino-8-oxo-7-azatridecanoate 
• 112507-71-8 13-benzyloxycarbonylamino-8-oxo-7-azatridecanoic acid hydrazide 
• 121759-91-9 p-nitrophenyl 13-benzyloxycarbonylamino-8-oxo-7-azatridecanoate 
• 109565-05-1 6-(6-amino-hexanoylamino)-hexanoic acid-(4-nitro-phenyl ester); hydrobromide 
• 108257-22-3 (5-{[(2R,3S,4R,5R)-5-(6-Amino-purin-9-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl]-carbamoyl}-pentyl)-carbamic acid benzyl ester 

Relevant academic research and scientific papers

Structure-Activity Relationship of 18F-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer

A series of phosphoramidate-based prostate specific membrane antigen (PSMA) inhibitors of increasing lipophilicity were synthesized (4, 5, and 6), and their fluorine-18 analogs were evaluated for use as positron emission tomography (PET) imaging agents for prostate cancer. To gain insight into their modes of binding, they were also cocrystallized with the extracellular domain of PSMA. All analogs exhibited irreversible binding to PSMA with IC50 values ranging from 0.4 to 1.3 nM. In vitro assays showed binding and rapid internalization (80-95%, 2 h) of the radiolabeled ligands in PSMA(+) cells. In vivo distribution demonstrated significant uptake in CWR22Rv1 (PSMA(+)) tumor, with tumor to blood ratios of 25.6:1, 63.6:1, and 69.6:1 for [18F]4, [18F]5, and [18F]6, respectively, at 2 h postinjection. Installation of aminohexanoic acid (AH) linkers in the phosphoramidate scaffold improved their PSMA binding and inhibition and was critical for achieving suitable in vivo imaging properties, positioning [18F]5 and [18F]6 as favorable candidates for future prostate cancer imaging clinical trials.

HEXADECASACCHARIDES WITH ANTITHROMBOTIC ACTIVITY, INCLUDING A COVALENT BOND AND AN AMINO CHAIN

The present invention relates to novel synthetic hexadecasaccharides with antithrombotic activity, having at least one covalent bond with an amino chain, and to the preparation method thereof and to the therapeutic use thereof.

In situ formation of N-trifluoroacetoxy succinimide (TFA-NHS): One-pot formation of succinimidyl esters, N-trifluoroacetyl amino acid succinimidyl esters, and N-maleoyl amino acid succinimidyl esters

A method for the in situ formation of N-trifluoroacetoxy succinimide (TFA-NHS) and its application in the formation of succinimidyl esters is presented. The developed method provides N-trifluoroacetyl and N-maleoyl amino acid succinimidyl esters from a variety of amino acids using a one-pot, high-yielding protocol. Investigations into the formation of an N-maleoyl amino acid succinimidyl ester supported the proposal of a revised reaction mechanism, and contributed to the optimization of the reaction conditions.

POLYSACCHARIDES WITH ANTITHROMBOTIC ACTIVITY, INCLUDING A COVALENT BOND AND AN AMINO CHAIN

The present invention relates to novel synthetic polysaccharides with antithrombotic activity, having at least one covalent bond with an amino chain, and to the preparation method thereof and to the therapeutic use thereof.

Branched supramolecular polymers formed by bifunctional cyclodextrin derivatives

Branched supramolecular polymers have been prepared from the mixture of 3-cinnamamide-α-CD (1) and 3-Nα-cinnamamidehexancarbonyl-Nε-cinnamamide-lysinamide-α-CD (3) and from the mixture of 3-cinnamamidehexanamide-α-CD (2) and 3. Compo

Design and photophysical properties of new RGD targeted tetraphenylchlorins and porphyrins

The synthesis, characterization, fluorescence, and singlet oxygen quantum yields of tetraphenylporphyrin and tetraphenylchlorin coupled to RGD type peptide are reported. C-terminus protected RGD derivatives were synthesized in liquid phase at the gram scale via an efficient convergent process. C-terminus unprotected RGD derivatives were synthesized on solid support. The UV-vis, fluorescence, and singlet emission spectra showed that the photophysical properties of the photosensitizers were retained in all compounds and some of them are very promising for potential PDT applications.

Supramolecular polymers formed by bifunctional cyclodextrin derivatives

The mixture of monofunctional and bifunctional cyclodextrin derivatives formed branched supramolecular polymers, which showed an increase in the viscosity of aqueous solution. However, a monofunctional cyclodextrin derivative did not form viscous solution

SYNTHESIS OF AZA-CROWN COMPOUNDS BY INTRAMOLECULAR CYCLIZATION OF ω-AMINO ACIDS

A method for the synthesis of aza-crown compounds by the intramolecular cyclization of ω-amino acids with subsequent reduction of the lactam to a macrocyclic amine was developed. 1,8-Diazacyclotetradecane and 1,8-dioxa-4,11-diazacyclotetradecane was synthesized in preparative yields.The structural assignments were made using the IR, 1H and 13C NMR, and mass spectra.

STUDIES ON LACTAMS IX. A CONVENIENT SYNTHESIS OF LACTAM RINGS

The auto-cyclization reaction has been employed for the synthesis of lactam rings by means of reduction from ω-carbobenzoxyamino acid active esters in high dilution method.