112157-30-9

Upstream product

• 7533-40-6 (S)-2-amino-4-methylpentan-1-ol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 61-90-5 L-leucine 
• 13139-15-6 N-tert-butoxycarbonyl-L-leucine 
• 82010-31-9 (S)-(1-hydroxymethyl-3-methylbutyl)carbamic acid tert-butyl ester 
• 98-59-9 p-toluenesulfonyl chloride 
• 63096-02-6 N-tert-butoxycarbonyl-L-leucine methyl ester 
• 2666-93-5 (S)-Leu-OMe 

Downstream Products

• 112383-35-4 Leu-Ψ(CH2S)-Ala-Aznva-OCH2Ph hydrochloride 
• 112383-10-5 N-<(1S)-(1-methoxycarbonyl-3-methylbutyl)carbamoyl>-L-leucyl-Ψ(CH2S)-L-alanyl-α-azanorvaline benzyl ester 
• 112383-34-3 N-t-butoxycarbonyl-L-leucyl-Ψ(CH2S)-L-alanyl-α-azanorvaline benzyl ester 
• 112157-36-5 (S)-2-Amino-N-{(S)-1-[(S)-2-((S)-2-amino-3-phenyl-propionylamino)-4-methyl-pentyldisulfanylmethyl]-3-methyl-butyl}-3-phenyl-propionamide; compound with trifluoro-acetic acid 
• 112157-34-3 ((S)-1-{(S)-1-[(S)-2-((S)-2-tert-Butoxycarbonylamino-3-phenyl-propionylamino)-4-methyl-pentyldisulfanylmethyl]-3-methyl-butylcarbamoyl}-2-phenyl-ethyl)-carbamic acid tert-butyl ester 
• 112157-33-2 (H-Leu(CH₂S)-)2*2HCl 
• 215608-35-8 methyl (S)-4-<(benzyloxycarbonyl)amino>-6-methyl-2-oxoheptanoate 
• 118247-68-0 N-Benzyloxycarbonyl-L-Homoleucine 
• 22818-43-5 (S)-3-amino-5-methylhexanoic acid 
• 1185454-00-5 C₁₂H₁₈BrNS 
• 1185453-88-6 C₁₇H₂₆BrNO₂S 
• 302800-26-6 (S)-2-amino-1-(dimethylamino)-4-methylpentane 
• 354988-10-6 (5S)-7-methyl-5-[N-(2-nitrophenylsulfonyl)amino]octa-1,2-diene 

Relevant academic research and scientific papers

The effect of urea moiety in amino acid binding by β-cyclodextrin derivatives: A 1000-fold increase in efficacy comparing to native β-cyclodextrin

Water soluble amphiphilic anion receptors based on urea-substituted β-cyclodextrin were synthesized via a copper(I) mediated azide-alkyne coupling reaction. The synthetic route was designed to minimize the number of operations of cyclodextrins. Stable pro

Synthesis and renin inhibitory activity of angiotensinogen analogues having dehydrostatine, Leuψ[CH2S]Val, or Leuψ[CH2SO]Val at the P1-P1' cleavage site

The synthesis and in vitro renin inhibitory potencies of angiotensinogen (ANG) analogues having amide (CONH) bond replacements at P1-P1', the Leu-Val cleavage site, corresponding to Leuψ[CH2S]Val, Leuψ[CH2SO]Val

Design, synthesis, and structure-activity relationship studies of L-amino alcohol derivatives as broad-spectrum antifungal agents

To discover broad spectrum antifungal agents, two strategies were applied, and a novel class of L-amino alcohol derivatives were designed and synthesized. 3-F substituted compounds 14i, 14n, 14s and 14v exhibited excellent antifungal activities with broad antifungal spectra against C. albicans and C. tropicalis, with MIC values in the range of 0.03–0.06 μg/mL, and against A. fumigatus and C. neoformans, with MIC values in the range of 1–2 μg/mL. Notably, Compounds 14i, 14n, 14s and 14v also displayed moderate activities against fluconazole-resistance strains 17# and CaR that were isolated from AIDS patients. Moreover, only compounds in the S-configuration showed antifungal activity. Preliminary mechanistic studies showed that the potent antifungal activity of compound 14v stemmed from inhibition of C. albicans CYP51. Compounds 14n and 14v were almost nontoxic to mammalian A549 cells, and their stability in human plasma was excellent.

A rapid entry to amino acid derived diverse 3,4-dihydropyrazines and dihydro[1,2,3]triazolo[1,5-a]pyrazines through 1,3-dipolar cycloaddition

An efficient, general and practical synthesis of diverse 3,4-dihydropyrazines, 6,7-dihydro-[1,2,3]triazolopyrazines and 7,8-dihydro-[1,2,3]triazolodiazepines through intramolecular 1,3-dipolar cycloaddition from amino acid derived common intermediates with high yields is described. Moreover, one-pot access to optically active 3-aryl substituted 6,7-dihydro-[1,2,3]triazolo[1,5-a]pyrazines in the palladium-copper co-catalytic system has also been achieved in this work. The easy substrate availability and operational simplicity make the process suitable for further exploration. This journal is the Partner Organisations 2014.

BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES AS APJ RECEPTOR MODULATORS

The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R', R", R"', R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The comp

BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES AS APJ RECEPTOR MODULATORS

The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R′, R″, R′″, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The comp

Syntheis of new chiral 5,6,7,8-tetrahydrotetrazolo[1,5-a]pyrazines from α-amino acid derivatives following "click" chemistry

An efficient and practical synthesis of new chiral fused tetrazoles have been synthesized following [3+2] cycloaddition reaction starting from α-amino acid derivatives.

Synthesis of new chiral 4,5,6,7-tetrahydro[1,2,3]triazolo[1,5-a]pyrazines from α-amino acid derivatives under mild conditions

A practical and efficient regioselective synthesis of several new chiral 4,5,6,7-tetrahydro[1,2,3]triazolo[1,5-a]pyrazines is described from α-amino acid derivatives following intramolecular 'click' reaction as the key step. The method obviates product pu

Stereoselective synthesis of 2-alkenylaziridines and 2-alkenylazetidines by palladium-catalyzed intramolecular amination of α- and β-amino allenes

Whereas palladium-catalyzed reaction of N-arylsulfonyl-α-amino allenes with an aryl iodide (4 equiv) in the presence of potassium carbonate (4 equiv) in DMF at around 70 °C affords the corresponding 3-pyrroline derivatives, the reaction in refluxing 1,4-dioxane under otherwise identical conditions yields exclusively or most predominantly the corresponding 2-alkenylaziridines bearing an aryl group on the double bond. Similarly, N-arylsulfonyl-β-amino allenes can be also cyclized into the corresponding alkenylazetidines bearing a 2,4-cis-configuration under palladium-catalyzed cyclization conditions in DMF.

New chiral auxiliaries for the construction of quaternary stereocenters by copper-catalyzed Michael reactions

The construction of quaternary stereocenters with 95-99% ee at ambient temperatures can be achieved by a copper-catalyzed Michael reaction with the application of α-amino acid amides as chiral auxiliaries [Eq. (1)]. These amides can be obtained in a few steps from the α-amino acids with standard transformations and, after the Michael reaction, they can be quantitatively recovered. Exclusion of water and oxygen is not necessary.