158141-67-4

Upstream product

• 75-65-0 tert-butyl alcohol 
• 1947-00-8 6-(benzyloxycarbonylamino)hexanoic acid 
• 98946-18-0 tert-Butyl 2,2,2-trichloroacetimidate 
• 501-53-1 benzyl chloroformate 
• 60-32-2 6-aminohexanoic acid 
• 115-11-7 isobutene 

Downstream Products

• 1353744-96-3 C₃₅H₄₂N₂O₆ 
• 1353744-95-2 benzyl 2-(5-(tert-butoxycarbonyl)pentylamino)ethylcarbamate 
• 5514-98-7 6-aminohexanoic acid tert-butyl ester 
• 158141-63-0 N-<5-(tert-Butyloxycarbonyl)pentyl>-4,5-bisamino>valeramide 
• 158141-64-1 N-(5-Carboxypentyl)-4,5-bisamino>valeramide 
• 158141-61-8 N-<5-(tert-Butyloxycarbonyl)pentyl>-4,5-bis<(benzyloxycarbonyl)amino>valeramide 
• 185426-28-2 6-(Benzyl-benzyloxycarbonylmethyl-amino)-hexanoic acid tert-butyl ester 
• 185426-12-4 6-Benzylamino-hexanoic acid tert-butyl ester 

Relevant academic research and scientific papers

Synthesis of camptothecin melantotransferrin (p97) conjugate through a carbamate bond

Through its 20-hydroxy group and a carbamate bond, 20(S)-camptothecin (1) is chemically linked to melanotransferrin (p97). The key step to modify the steric hindered hydroxy group of camptothecin is achieved by using triphosgene/DMAP in DMF and immediately reacting with tert-butyl 6-aminohexanoate (8). The novel camptothecin conjugate 4 is a potential agent for chemotherapy of brain tumor.

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERRα degraders to date. Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERRα.

A MedChem toolbox for cereblon-directed PROTACs

A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.

TRI-FUNCTIONAL CROSSLINKING REAGENTS

The present invention relates to tri-functional crosslinking reagents carrying (i) a ligand-reactive group for conjugation to a ligand of interest having at least one binding site on a target glycoprotein receptor, (ii) a hydrazone group for the capturing

CARBON MONOXIDE RELEASING NORBORNENONE COMPOUNDS

The present invention provides organic compounds which are capable of releasing carbon monoxide under physiological conditions or pH trigger, and to the use of such compounds for conditioning a cell, tissue or organ, for example, to protect against ischaemic injury during a transplant event.

QUINONE-MASKED PROBES AS LABELING REAGENTS FOR CELL UPTAKE MEASUREMENTS

Provided are labeling reagents and methods of using the reagents for cell uptake measurements. The labeling reagents can be quinone- masked probes including fluorophores and/or luminophores.

Carboxyalkyl peptoid PNAs: Synthesis and hybridization properties

Nγ-Carboxyalkyl modified peptide nucleic acids (PNAs), containing the four canonical nucleobases, were prepared via solid-phase oligomerization. The inserted peptoid monomers 1 and 2 were constructed through simple synthetic procedures, utilizi

IRINOTECAN IMMUNOASSAY

Novel conjugates of the pharmaceutically active metabolite of irinotecan and novel immunogens derived from this pharmaceutically active metabolite and monoclonal antibodies generated by these immunogens which are useful in immunoassays for the quantificat

SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASE

The present application relates to novel substituted bicyclic heteroaryl compounds, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or proph

Synthesis and self-association properties of flexible guanidiniocarbonylpyrrole-carboxylate zwitterions in DMSO: Intra- versus intermolecular ion pairing

(Chemical Equation Presented) We have synthesized a new class of flexible zwitterions 6a-e, in which a carboxylate is linked via an alkyl chain with variable length (one to five methylene groups) to a guanidiniocarbonylpyrrole cation. The self-association properties of these zwitterions were determined by NMR dilution studies in DMSO and by ESI-MS experiments. The stability and hence also the size of the aggregates formed via self-assembly is critically dependent on the length and therefore flexibility of the spacer. Whereas the smallest zwitterion 6a forms large aggregates already at low concentrations, the more flexible zwitterions only form small oligomers (6b) or dimers (6c-e) at much larger concentrations. The differences between the five zwitterions can be explained based on the different extent of intramolecular ion pairing within the monomers. Any intramolecular ion pairing, which becomes possible with increasing linker length, stabilizes the monomer and therefore destabilizes any oligomer.