298693-79-5

Upstream product

• 69942-12-7 N-tert-butoxycarbonylserine methyl ester 
• 623-00-7 4-bromobenzenecarbonitrile 
• 175844-11-8 methyl (2R)-2-[(tert-butoxycarbonyl)amino]-3-bromopropionate 
• 74-83-9 methyl bromide 
• 131724-45-3 (S)-2-((tert-butoxycarbonyl)amino)-3-(4-cyanophenyl)propanoic acid 
• 93267-04-0 N-(tert-butoxycarbonyl)-L-3-iodoalanine methyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 557-21-1 zinc(II) cyanide 
• 112766-18-4 methyl N-(tert-butoxycarbonyl)-O-[(trifluoromethyl)sulfonyl]-L-tyrosinate 
• 4326-36-7 (S)-N-(tert-butoxycarbonyl)tyrosine methyl ester 
• 266306-18-7 (S)-3-(4-Bromo-phenyl)-2-tert-butoxycarbonylamino-propionic acid methyl ester 
• 67-56-1 methanol 
• 151-50-8 potassium cyanide 

Downstream Products

• 1227311-10-5 methyl (S)-2-((tert-butoxycarbonyl)amino)-3-(4-cyano-2,6-dimethylphenyl)propanoate 
• 623950-05-0 methyl (S)-2-((tert-butoxycarbonyl)amino)-3-(4-carbamoyl-2,6-dimethylphenyl)propanoate 
• 207449-48-7 (S)-3-(4-Aminomethyl-phenyl)-2-(2-trimethylsilanyl-ethoxycarbonylamino)-propionic acid methyl ester 
• 207449-47-6 (S)-3-(4-Cyano-phenyl)-2-(2-trimethylsilanyl-ethoxycarbonylamino)-propionic acid methyl ester 
• 216774-50-4 N-tert-butyloxycarbonyl-(p-hydroxymethyl)-L-phenylalanine methyl ester 
• 206060-45-9 N-(fluorenyl-9-methoxycarbonyl)-L-(p-sulfomethyl)phenylalanine 
• 945245-54-5 N-(fluorenyl-9-methoxycarbonyl)-L-(p-sulfomethyl)phenylalanyl-L-(4-O-benzyl)-aspartic acid α-tert-butyl ester 

Relevant academic research and scientific papers

Synthesis of Enantiopure Unnatural Amino Acids by Metallaphotoredox Catalysis

We describe herein a two-step process for the conversion of serine to a wide array of optically pure unnatural amino acids. This method utilizes a photocatalytic cross-electrophile coupling between a bromoalkyl intermediate and a diverse set of aryl halides to produce artificial analogues of phenylalanine, tryptophan, and histidine. The reaction is tolerant of a broad range of functionalities and can be leveraged toward the scalable synthesis of valuable pharmaceutical scaffolds via flow technology.

Design, synthesis, and evaluation of a novel benzamidine-based inhibitor of VEGF-C binding to Neuropilin-2

The Neuropilin (Nrp) family of cell surface receptors have key physiological and pathological functions. Nrp2 is of particular interest due to its involvement in tumor metastasis. Currently, peptide and small molecule inhibitors that target Nrp utilize ar

OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO

Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R3, R4, R5, R6, R8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.

Preparation method of alanine derivatives

The invention discloses a method for preparing alanine derivatives disclosed as Formula (I). The alanine derivatives can be used as a synthesis intermediate of an opioid receptor regulator, such as a synthesis intermediate of eluxadoline. By using the cheap and accessible chiral tyrosine as the initial raw material, the invention provides a brand-new synthesis route for preparing alanine derivatives. The whole reaction route has the advantages of high total yield, low cost and mild reaction conditions, is simple and safe for operation, and is suitable for large-scale industrial production.

Mild palladium-catalyzed cyanation of (hetero)aryl halides and triflates in aqueous media

A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.

Synthesis of isotopomers of N-(tert-butoxycarbonyl)-4-cyano-l-phenylalanine methyl ester: Choice of cyanation solvent

N-(tert-butoxycarbonyl)-4-cyano-l-phenylalanine methyl ester and three isotopomers (C15N, 13CN, and 13C15N) were successfully synthesized in two steps to expand the utility of the nitrile symmetric stretch vibra

(p-Sulfomethyl)phenylalanine as a mimic of O-sulfatyl-tyrosine in synthetic partial sequences of P-Selectin glycoprotein ligand 1 (PSGL-1)

Fmoc-l-(p-sulfomethyl)phenylalanine, a bioisosteric mimic of acid-sensitive O-sulfatyl tyrosine, was synthesized from l-tyrosine according to a novel route. Partial sequences of the recognition site of P-Selectin glycoprotein ligand 1 (PSGL-1), which cont

NOVEL HYDROXAMIC ACID DERIVATIVES

Disclosed are compounds which have not only potent metalloproteinase-inhibiting activity but also amazingly excellent bioavailability and biological activity invivo, including the property of being well absorbed via oral routes, thereby serving as useful pharmaceuticals, intermediates and processes for the production thereof. The disclosed compounds of the formula (I): wherein R1 is hydrogen, or a hydroxy-protecting group; R2 is hydrogen, or an amino-protecting group; R3, R7, and R8, which may be identical or different, are each independently hydrogen, hydroxy, unsubstituted or optionally substituted (C1-C6) alkyl, or unsubstituted or optionally substituted aryl-(C1-C6) alkyl; R4 is unsubstituted or optionally substituted (C1-C6) alkyl, or unsubstituted or optionally substituted aryl-(C1-C6) alkyl; R5 is hydrogen, unsubstituted or optionally substituted alkyl, unsubstituted or optionally substituted aralkyl, or a carboxy-protecting group; R6 is hydrogen, hydroxy, amino, and a group of the formula: -X-Y wherein X is oxygen, (C1-C6) alkylene or phenylene, Y is a group of the formula: -A-B or -B, wherein A is (C1-C6) alkylene, imino, and (C1-C6) alkyleneimino, and B is hydrogen, amino, amidino, sulfonyl, acylimidoyl, unsubstituted or optionally substituted imidazolyl, unprotected or optionally protected bis(phosphono)methyl or unprotected or optionally protected bis(phosphono)hydroxymethyl; or salts thereof are useful for pharmaceutical and/or veterinary compositions, particularly as metalloproteinase inhibitors which inhibit matrix metalloproteinases or tumor necrosis factor-α-converting enzymes (TNF-α convertases).

Process for synthesizing para-and/or meta-substituted cyanophenyalanine derivatives

The present invention relates to a process for preparing a useful medicinal intermediate represented by the following formula (1): in which, R1, A and n are defined as described in the specification, or its stereoisomer, characterized in that a

Process for synthesizing para-and/or meta-substituted cyanophenylalanine derivatives

The present invention relates to a process for preparing a useful medicinal intermediate represented by the following formula (1): ???in which, R1, A and n are defined as described in the specification, or its stereoisomer, characterized in tha