354820-63-6

Upstream product

• 3195-65-1 methyl 3-nitro-L-tyrosinate 
• 621-44-3 3-nitro-L-tyrosine 
• 4326-36-7 (S)-N-(tert-butoxycarbonyl)tyrosine methyl ester 

Downstream Products

• 439253-51-7 (S)-2-tert-Butoxycarbonylamino-3-(4-hydroxy-3-{[1-pyridin-2-yl-meth-(E)-ylidene]-amino}-phenyl)-propionic acid methyl ester 
• 898224-71-0 (S)-2-tert-Butoxycarbonylamino-3-(4-hydroxy-3-{[1-quinolin-8-yl-meth-(E)-ylidene]-amino}-phenyl)-propionic acid methyl ester 
• 1058176-71-8 N-tert-butyloxycarbonyl 3-(bithien-2'-yl)imino-L-tyrosine methyl ester 
• 1058176-73-0 C₂₈H₂₈N₂O₅S₃ 
• 1058176-69-4 C₂₂H₂₆N₂O₇S 
• 650141-45-0 C₂₃H₂₆N₂O₅ 
• 1305308-73-9 C₂₂H₂₄N₂O₅ 
• 1402739-46-1 3-[2-(4-boronophenyl)benzoxazol-5-yl]alanine methyl ester 
• 1402739-45-0 N-Boc-3-[2-(3-boronophenyl)benzoxazol-5-yl]alanine methyl ester 
• 1402739-47-2 3-[2-(3-boronophenyl)benzoxazol-5-yl]alanine methyl ester 

Relevant academic research and scientific papers

Application of Nitroimidazole-Carbobane-Modified Phenylalanine Derivatives as Dual-Target Boron Carriers in Boron Neutron Capture Therapy

Boron neutron capture therapy (BNCT) has received extensive attention as noninvasive cell-level oncotherapy for treating solid cancer tumors. However, boron-containing drugs such as l-boronophenylalanine (BPA) and sodium borocaptate have low boron content

Synthesis of a New, Highly Fluorescent Amino Acid Derivative: N-[(tert-Butoxy)carbonyl]-3-[2-(1H-indol-3-yl)benzoxazol-5-yl]-L-alanine Methyl Ester

A simple method of synthesis of a new, highly fluorescent amino acid derivative from the simple and generally available substrates 3-nitro-L-tyrosine and 1H-indole-3-carbaldehyde is described. The obtained compound, N-[(tert-butoxy)carbonyl]-3-[2-(1H-indo

CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP

Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

Cu(II)-Mediated N-H and N-Alkyl Aryl Amination and Olefin Aziridination

Cu(II)-mediated direct NH2 and NH alkyl aryl aminations and olefin aziridinations are described. These room-temperature, one-pot, environmentally friendly procedures replace costly Rh2 catalysts and, in some instances, display important differences with comparable Rh2- and Fe-supported reactions.

CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE

What provided is the conjugation of cytotoxic to a cell-binding molecule with a bis-linker(dual-linker) as shown in Formula (I). It provides bis-linkage methods of making a conjugate of a cytotoxic drug molecule to a cell-binding agent in a specific manner. It also relates to application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.

Polyboron phenylalanine compound containing nitroimidazole, as well as preparation method and application thereof

The invention discloses a polyboron phenylalanine compound containing nitroimidazole as shown in a general formula (I) in the specification or pharmaceutically acceptable salt thereof, as well as a preparation method and application thereof. The compound

Quantitative insight into the design of compounds recognized by the L-type amino acid transporter 1 (LAT1)

L-Type amino acid transporter 1 (LAT1) is a transmembrane protein expressed abundantly at the blood-brain barrier (BBB), where it ensures the transport of hydrophobic acids from the blood to the brain. Due to its unique substrate specificity and high expression at the BBB, LAT1 is an intriguing target for carrier- mediated transport of drugs into the brain. In this study, a comparative molecular field analysis (CoMFA) model with considerable statistical quality (Q2=0.53, R2=0.75, Q2 SE=0.77, R2 SE=0.57) and good external predictivity (CCC=0.91) was generated. The model was used to guide the synthesis of eight new prodrugs whose affinity for LAT1 was tested by using an in situ rat brain perfusion technique. This resulted in the creation of a novel LAT1 prodrug with l-tryptophan as the promoiety; it also provided a better understanding of the molecular features of LAT1-targeted high-affinity prodrugs, as well as their promoiety and parent drug. The results obtained will be beneficial in the rational design of novel LAT1-binding prodrugs and other compounds that bind to LAT1.

Photophysical properties of 3-[2-(N-phenylcarbazolyl)benzoxazol-5-yl] alanine derivatives-experimental and theoretical studies

Solvatochromic probes are often used in biophysical studies to obtain information about polarity of the microenvironment. As there is not much natural fluorophores with such properties, there is still need for new synthetic compounds such as 3-(2-benzoxaz

3-[2-(Boronophenyl)benzoxazol-5-yl]alanine derivatives as fluorescent monosaccharide sensors

Two 3-[2-(boronophenyl)benzoxazol-5-yl]alanine derivatives were synthesized and their potential application as fluorescent monosaccharide sensors was studied. It was found that both non-proteinogenic amino acids bound glucose and fructose at physiological pH, however, the latter much stronger. As a result they are selective sensors for fructose. Moreover, one of them (3-[2-(3-boronophenyl)benzoxazol-5-yl]alanine methyl ester) can be used to quickly distinguish, which monosaccharide is present in the solution because of the different character of fluorescence intensity changes (increase in the presence of fructose and decrease in the presence of glucose).

A simple protocol for the synthesis of 2-arylbenzoxazoles by oxidation with o-iodoxybenzoic acid (IBX) and its application in the synthesis of arylbenzoxazole-containing amino acids

A simple protocol for the preparation of 2-arylbenzoxazoles has been developed based on the oxidation of phenolic Schiff bases with o-iodoxybenzoic acid (IBX), wherein the oxidant can be recycled. The robustness of this new protocol has been demonstrated in the synthesis of arylbenzoxazole-containing amino acids.