81677-61-4

Upstream product

• 81677-60-3 (L)-p-Nitrophenylalanine methyl ester 
• 33305-77-0 Boc-Phe(p-NO₂)-OH 
• 17193-40-7 (S)-4-nitrophenylalanine methyl ester hydrochloride 
• 63-91-2 L-phenylalanine 
• 949-99-5 4-nitro-3-phenyl-L-alanine 
• 66163-67-5 [1-(S)-carbamoyl-2-(4-nitrophenyl)ethyl]carbamic acid tert-butyl ester 

Downstream Products

• 365431-39-6 Fmoc-Orn(Boc)-Phe(4NO₂)-NH₂ 
• 1599422-83-9 2-{(2S)-1-[4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl]-3-(4-nitrophenylpropan-2-yl)amino}acetic acid 
• 1599422-87-3 (2S)-1-(4-nitrophenyl)-3-(1,4,7-triazonan-1-yl)propan-2-amine 
• 1599422-88-4 tert-butyl 2-{[(2S)-1-{4,7-bis[2-(tert-butoxy)-2-oxoethyl]-1,4,7-triazonan-1-yl}-3-(4-nitrophenyl)propan-2-yl]amino}acetate 
• 143106-46-1 tetra-tert-butyl 2,2',2”,2”'-((3-(4-aminophenyl)propane-1,2-diyl)bis(azanetriyl))tetraacetate 
• 1599422-84-0 (2S)-2-[(4-methylphenyl)sulfonamido]-3-(4-nitrophenyl)propanamide 
• 1599422-86-2 N-{(2S)-1-[4,7-bis(4-methylphenylsulfonyl)-1,4,7-triazonan-1-yl]-3-(4-nitrophenyl)propan-2-yl}-4-methylbenzene-1-sulfonamide 
• 1599422-85-1 N-[(2S)-1-amino-3-(4-nitrophenyl)propan-2-yl]-4-methylbenzene-1-sulfonamide 
• 365431-63-6 cyclo[Pmp-Tyr-Ile-Thr-Asn-Cys]-Pro-Orn(Boc)-Phe(3I,4N₃)-NH₂ 
• 365431-62-5 cyclo[Pmp-Tyr(Me)-Ile-Thr-Asn-Cys]-Pro-Orn(Boc)-Phe(3I,4N₃)-NH₂ 
• 365431-60-3 cyclo[Pmp-Tyr(Me)-Ile-Thr-Asn-Cys]-Gly-Orn(Boc)-Phe(3I,4N₃)-NH₂ 
• 365431-61-4 cyclo[Pmp-Tyr-Ile-Thr-Asn-Cys]-Gly-Orn(Boc)-Phe(3I,4N₃)-NH₂ 
• 365431-46-5 H-Orn(Boc)-Phe(3I,4N₃)-NH₂ 
• 365431-44-3 H-Orn(Boc)-Phe(3I,4NH₂)-NH₂ 

Relevant academic research and scientific papers

Small molecule macroarray construction via Ugi four-component reactions

(Chemical Equation Presented) We report the construction of small molecule macroarrays via Ugi four-component reactions on planar cellulose supports. Array synthesis was enabled by the development of a high efficiency photocleavable linker system and the

Specific molecular marked heavy-metal chelating agent, corresponding rapid chromatographic detection card and application

The invention relates to a specific molecular marked heavy-metal chelating agent, corresponding detection technologies and application. The heavy-metal chelating agent disclosed by the invention is metal chelating molecules marked by specific marking molecules; after being combined with heavy metal, one ends of the molecules can be identified and captured by an antibody; the marking molecules at the other ends are combined with a corresponding ligand or antibody; therefore, sandwich detection is realized; and the detection technologies comprise an enzyme-linked immune technology and a rapid paper chromatographic technology. By means of the specific molecular marked heavy-metal chelating agent, the corresponding detection technologies and application disclosed by the invention, rapid sandwich detection on metal ion can be realized for the first time; requirements of conventional heavy-metal detection on an expensive instrument can be avoided; and thus, disadvantages of the sensitivity and the specificity of a competition-method heavy-metal rapid detection card can be made up.

Synthesis and evaluation of an enantiomerically enriched bifunctional chelator for 64Cu-based positron emission tomography (PET) imaging

We report the synthesis and evaluation of an enantiomerically enriched bifunctional chelator, (S)-C-NE3TA. The bifunctional chelator was efficiently prepared by regioselective and stereoselective ring opening of an aziridinium ion. The new chiral chelator instantly and almost completely bound to 64Cu at room temperature. The corresponding 64Cu- radiolabeled complex remained intact in human serum for 48 h without any measurable transchelation and was tolerant to a rigorous EDTA challenge for 24 h. The 64Cu-radiolabeled (S)-C-NE3TA complex was stable in mice and produced an excellent biodistribution profile. The results of the in vitro and in vivo evaluations indicate that the new optically active chelator is a promising candidate for PET imaging applications. We report an enantiomerically enriched bifunctional ligand in the NE3TA series for the first time. The chelator instantly bound to 64Cu to form a complex that was stable in vitro and in vivo and possesses great promise for use in targeted positron emission topography (PET) imaging. Copyright

Synthesis and Evaluation of an Enantiomerically Enriched Bifunctional Chelator for 64Cu-Based Positron Emission Tomography (PET) Imaging

We report the synthesis and evaluation of an enantiomerically enriched bifunctional chelator, (S)-C-NE3TA. The bifunctional chelator was efficiently prepared by regioselective and stereoselective ring opening of an aziridinium ion. The new chiral chelator instantly and almost completely bound to 64Cu at room temperature. The corresponding 64Cu-radiolabeled complex remained intact in human serum for 48 h without any measurable transchelation and was tolerant to a rigorous EDTA challenge for 24 h. The 64Cu-radiolabeled (S)-C-NE3TA complex was stable in mice and produced an excellent biodistribution profile. The results of the in vitro and in vivo evaluations indicate that the new optically active chelator is a promising candidate for PET imaging applications.

Indole nitriles

Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.

Synthesis of novel bifunctional Schiff-base ligands derived from condensation of 1-(p-nitrobenzyl)ethylenediamine and 2-(p-nitrobenzyl)-3-monooxo-1,4,7-triazaheptane with salicylaldehyde

Two potentially tetradentate (N2O2) and pentadentate (N3O3) bifunctional Schiff-base ligands, N,N′-bis(2-hydroxybenzyl)-1-(p-aminobenzyl)ethylenediamine (7) and N,N′-bis(2-hydroxybenzyl)-2-(p-aminobenzyl)-3-monooxo-1,4,7- triazaheptane (5′) have been prepared and characterized by various spectroscopic methods (IR, FAB-MS, NMR). They are derived from the condensation reactions of the C-functionalized diamines 1-(p-nitrobenzyl)ethylenediamine and 2-(p-nitrobenzyl)-3-monooxo-1,4,7-triazaheptane with 2.1 equiv. of salicylaldehyde. The first complexation trials with 99mTc are reported.

Design, synthesis and pharmacological characterization of a potent radioiodinated and photoactivatable peptidic oxytocin antagonist

Using a segment strategy, we have synthesized four iodinated photoactivatable cyclic peptidic ligands of oxytocin, bearing a β-mercapto-ββ-cyclopentamethylene propionic group (Pmp) on their N-terminus. All the syntheses were RP-HPLC monitored, and the com