15136-26-2

Upstream product

• 28140-49-0 L-Val-D,L-Ala-OCH₃ 
• 72-18-4 L-valine 
• 24601-74-9 (S)-4-isopropyloxazolidine-2,5-dione 
• 113304-69-1 IPAoc-Ala-Val-OSu 
• 99474-03-0 L-Val-L-Ala-OEt 
• 77946-33-9 Boc-Val-Ala-OBzl 
• 2491-20-5 L-alanine methyl ester hydrochloride 
• 68858-20-8 Fmoc-Val-OH 
• 35661-39-3 N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-alanine 
• 84255-92-5 L-Alanyl-L-valine Methyl Ester 
• 4864-38-4 (S)-2-((S)-2-Benzyloxycarbonylamino-propionylamino)-3-methyl-butyric acid methyl ester 
• 870764-59-3 benzyloxycarbonyl-alanyl-valine 
• 13734-41-3 t-Boc-L-valine 
• 1203578-13-5 4-N-[Nα-(benzyloxycarbonyl)valylalanyl]-1-β-D-arabinofuranosylcytosine 

Downstream Products

• 81136-86-9 (3S,6S,R)-2,5-Dimethoxy-3-isopropyl-6-methyl-3,6-dihydropyrazine 
• 84907-75-5 (2R,5S)-2,5-dihydro-5-isopropyl-3,6-dimethoxy-2-methyl-2-(1'-phenylethenyl)-pyrazine 
• 88050-50-4 (3R,6S)-3-(2-benzylthioethyl)-6-isopropyl-2,5-dimethoxy-3-methyl-3,6-dihydropyrazine 
• 83537-81-9 (3R,6S)-3-[(benzyloxy)methyl]-6-isopropyl-1,4-dimethoxy-3-methyl-3,6-dihydropyrazine 
• 84907-70-0 1-((2R,5S)-5-Isopropyl-3,6-dimethoxy-2-methyl-2,5-dihydro-pyrazin-2-yl)-1-phenyl-ethanol 
• 81136-87-0 (2S,5R)-2,5-dihydro-2-isopropyl-3,6-dimethoxy-5-benzyl-5-methylpyrazine 
• 81136-89-2 (2R,5S)-5-Isopropyl-3,6-dimethoxy-2-methyl-2-((E)-3-phenyl-allyl)-2,5-dihydro-pyrazine 
• 81136-88-1 (2R,5S)-2-(3,4-Dimethoxy-benzyl)-5-isopropyl-3,6-dimethoxy-2-methyl-2,5-dihydro-pyrazine 
• 17609-47-1 L-Valine ethyl ester hydrochloride 
• 72-18-4 L-valine 

Relevant academic research and scientific papers

Preparation of novel 2-(trialkylsilyl)ethyl linkers and first synthesis of Tryprostatin B on solid phase

Two synthetic methods for novel polymer-supported 2-(trialkylsilyl)ethanol linkers 3 are described. The new silyl linker has been examined as a C-terminal linkage to provide several diketopiperazines. Using this synthetic method, the first solid phase synthesis of Tryprostatin B was accomplished. Several functionalized 2-(trialkylsilyl)ethyl linkers 12-17 are synthesized from 2-(trialkylsilyl)ethanol linkers. During the course of preparations, the new silyl linkers proved resistant to various reaction conditions such as basic and moderately acidic media, oxidation, and elevated thermal conditions.

SUBSTITUTED NAPHTHYRIDINONE COMPOUNDS USEFUL AS T CELL ACTIVATORS

Disclosed are compounds of Formula (I) or a salt thereof, wherein: R1, R2, R3, R4, R5, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα) and diacylglycerol kinase zeta (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

Anti-biofilm and anti-adherence properties of novel cyclic dipeptides against oral pathogens

Microorganisms embedded in a biofilm are significantly more resistant to antimicrobial agents and the defences of the human immune system, than their planktonic counterpart. Consequently, compounds that can inhibit biofilm formation are of great interest for novel therapeutics. In this study, a screening approach was used to identify novel cyclic dipeptides that have anti-biofilm activity against oral pathogens. Five new active compounds were identified that prevent biofilm formation by the cariogenic bacterium Streptococcus mutans and the pathogenic fungus Candida albicans. These compounds also inhibit the adherence of microorganisms to a hydroxylapatite surface. Further investigations were conducted on these compounds to establish the structure–activity relationship, and it was deduced that the common cleft pattern is required for these molecules to act effectively against biofilms.

Application of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to different amine-containing drugs

Here we explore the applicability of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to a variety of amine-containing drugs. Efficient procedures have been developed for the synthesis of dipeptide and tetrapeptide amide prodrugs including

Structures, sensory activity, and dose/response functions of 2,5-diketopiperazines in roasted cocoa nibs (Theobroma cacao)

The taste compounds inducing the blood-like, metallic bitter taste sensation reported recently for a dichloromethane extract prepared from roasted cocoa nibs were identified as a series of 25 diketopiperazines by means of HPLC degustation, LC-MS/MS, and i

SYNTHESIS OF (2R)- AND (2S)- -2-AMINO-2-METHYLMALONIC ACID: CHIRAL SUBSTRATES FOR SERINE HYDROXYMETHYLTRANSFERASE

(2R)- and (2S)--2-amino-2-methylmalonate, probes for the stereochemical course of the serine hydroxymethyltransferase reaction, have been synthesised from bis-lactim ethers derived from valine and alanine.Direct acylation of the anion with diethyl carbonate gave the N-ethoxycarbonyl derivative rather than the required ethyl ester.The 13C-labelled carboxyl group was therefore introduced via treatment of the anion with -acetyl chloride, followed by haloform oxidation.The resulting carboxylate salt was then esterified with methyl iodide, and the bis-lactither ring system was cleaved under acidic conditions to give the amino acid esters.Saponification and then separation by cation chromatography gave the title compounds.

1-ISOPROPYLALLYLOXYCARBONYL (IPAoc) AS A PROTECTIVE GROUP OF AMINES AND ITS DEPROTECTION CATALYSED BY PALLADIUM-PHOSPHINE COMPLEX

As a new protective group of amines, 1-isopropylallyloxycarbonyl (IPAoc) group was developed.IPAoc group can be removed by treatment with a palladium-phosphine catalyst forming carbon dioxide and 4-methyl-1,3-pentadiene by the decarboxylation and β-hydrogen elimination of (?-1-isopropylallyl)-palladium intermediate under neutral condititons.The present protection-deprotection was applied to a one-pot peptide synthesis.

Synthesis of "Chiral" α-Aminoisobutyric Acid

α-Methylalanine (α-aminoisobutyric acid), a rare naturally occuring achiral amino acid, is an efficient inducer of secondary structure for peptides and easy to characterize by NMR because of its prochiral methyl groups. "Chiral" α-methylalanine is enantioselectively synthesized via the bislactim-ether method where the pro-R-methyl group has three or one deuterium atom(s).

ENANTIOSELECTIVE SYNTHESIS OF NON-PROTEINOGENIC AMINO ACIDS VIA METALLATED BIS-LACTIM ETHERS OF 2,5-DIKETOPIPERAZINES

Bis-lactim ethers 1 of 2,5-diketopiperazines contain a chiral inducing center, an acidic CH-bond and two sites susceptible to hydrolysis.They react with BuLi to give Li compounds of type 4, 15, 29 or 32, which possess a prochiral C atom.They readily add electrophiles (such as alkylating agents or carbonyl compounds) with unusually high diastereoface differentiation.In many cases the d.e-value (d.e. = diastereomeric excess = asymmetric induction) of the adduct exceeds 95percent.On hydrolysis the adducts are cleaved liberating the chiral auxiliary (used to build up the bis-lactim ether 1) and the target molecules, the optically active amino acid methyl esters of type 8, 19, 25 or 36.The two amino acid esters are separable either by fractional distillation or (eventually after further hydrolysis to amino acids) by chromatography.Transition state models are discussed that could explain the exceptionally high asymmetric induction and the predictability of the induced configuration.