57746-16-4

Upstream product

• 50-00-0 formaldehyd 
• 1080-06-4 L-Tyr-OMe 
• 3417-91-2 L-tyrosine methyl ester HCl 
• 60-18-4 L-tyrosine 
• 1260499-43-1 methyl (S)-N,N-dimethyl-O-(tert-butyldimethylsilyl)tyrosinate 

Downstream Products

• 613263-91-5 methyl (S)-2-(dimethylamino)-3-(4-(((trifluoromethyl)sulfonyl)oxy)phenyl)propanoate 
• 613263-92-6 Trifluoro-methanesulfonic acid 4-((S)-2-dimethylamino-3-hydroxy-3-methyl-butyl)-phenyl ester 
• 1260499-43-1 methyl (S)-N,N-dimethyl-O-(tert-butyldimethylsilyl)tyrosinate 
• 1260499-44-2 (S)-3-[4-(tert-butyldimethylsilyloxy)phenyl]-2-(N,N-dimethylamino)-N-methoxy-N-methylpropanamide 
• 1260499-46-4 (2RS,6E,8R,10R)-1-[4-(tert-butyldimethylsilyloxy)phenyl]-2-(N,N-dimethylamino)-8,10-dimethyldodec-6-en-3-one 
• 1260540-26-8 (2RS,6E,8R,10R)-2-(N,N-dimethylamino)-1-(4-hydroxyphenyl)-8,10-dimethyldodec-6-en-3-one 

Relevant academic research and scientific papers

Discovery of Modified Amidate (ProTide) Prodrugs of Tenofovir with Enhanced Antiviral Properties

This study describes the discovery of novel prodrugs bearing tyrosine derivatives instead of the phenol moiety present in FDA-approved tenofovir alafenamide fumarate (TAF). The synthesis was optimized to afford diastereomeric mixtures of novel prodrugs in

Palladium-Catalyzed Chlorocarbonylation of Aryl (Pseudo)Halides Through In Situ Generation of Carbon Monoxide

An efficient palladium-catalyzed chlorocarbonylation of aryl (pseudo)halides that gives access to a wide range of carboxylic acid derivatives has been developed. The use of butyryl chloride as a combined CO and Cl source eludes the need for toxic, gaseous carbon monoxide, thus facilitating the synthesis of high-value products from readily available aryl (pseudo)halides. The combination of palladium(0), Xantphos, and an amine base is essential to promote this broadly applicable catalytic reaction. Overall, this reaction provides access to a great variety of carbonyl-containing products through in situ transformation of the generated aroyl chloride. Combined experimental and computational studies support a reaction mechanism involving in situ generation of CO.

Asymmetric Total Synthesis and Evaluation of Antitumor Activity of Ophiorrhisine A and Its Derivatives

The first asymmetric total synthesis of ophiorrhisine A (1), a new cyclic tetrapeptide isolated from Ophiorrhiza nutans, was accomplished via an intramolecular aromatic nucleophilic substitution reaction (IMSNAr) of a linear tripeptide to construct a 14-membered paracyclophane ring, resulting in confirmation of its structure and absolute configuration. The structure-activity relationship study of 1 and its derivatives demonstrated that some derivatives possessed cytotoxicity toward human cancer cell lines A549, HT29, and HCT116.

Expedient Synthesis of N-Methyl- and N-Alkylamines by Reductive Amination using Reusable Cobalt Oxide Nanoparticles

N-Methyl- and N-alkylamines represent important fine and bulk chemicals that are extensively used in both academic research and industrial production. Notably, these structural motifs are found in a large number of life-science molecules and play vital roles in regulating their activities. Therefore, the development of convenient and cost-effective methods for the synthesis and functionalization of amines by using earth-abundant metal-based catalysts is of scientific interest. In this regard, herein we report an expedient reductive amination process for the selective synthesis of N-methylated and N-alkylated amines by using nitrogen-doped, graphene-activated nanoscale Co3O4-based catalysts. Starting from inexpensive and easily accessible nitroarenes or amines and aqueous formaldehyde or aldehydes in the presence of formic acid, this cost-efficient reductive amination protocol allows the synthesis of various N-methyl- and N-alkylamines, amino acid derivatives, and existing drug molecules.

Synthesis of (2RS,8R,10R)-YM-193221 and an improved approach to tyroscherin, bioactive natural compounds from pseudallescheria sp

Short-step syntheses of (2RS,8R,10R)-YM-193221 (1) and tyroscherin (2), which are biologically active compounds isolated from Pseudallescheria sp., were accomplished in six and eight steps from L-tyrosine. The relative stereochemistry of natural YM-193221 was determined to be 8R*,10*.

Polypeptide compound and a process for preparation thereof

A polypeptide compound having antimicrobial activity of the following general formula: STR1 wherein R1 is hydrogen or acyl group, R2 is hydroxy or acyloxy, R3 is hydroxysulfonyloxy, and R4 is hydrogen or carbamoyl, with proviso that R1 is not palmitoyl, when R2 is hydroxy, R3 is hydroxysulfonyloxy and R4 is carbamoyl, and a pharmaceutically acceptable salt thereof.