81323-58-2

Upstream product

• 59768-74-0 (S)-2-t-butoxycarbonylaminosuccinic acid 4-methyl ester 
• 34582-31-5 1-tert-butyl 4-methyl (S)-2-{[(tert-butoxy)carbonyl]amino}butanedioate 
• 98946-18-0 tert-Butyl 2,2,2-trichloroacetimidate 
• 41088-86-2 L-2-(tert-butyloxycarbonylamino)-4-hydroxybutyric acid 
• 672-15-1 L-homoserine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 507-19-7 t-butyl bromide 
• 215182-75-5 (2S)-tert-butyl 2-[N-(9-(9-phenylfluorenyl))amino]-4-hydroxybutanoate 
• 80963-08-2 N-tert-butoxycarbonyl-L-aspartic acid β-benzyl α-tert-butyl diester 
• 7536-58-5 BOC-L-aspartic acid 4-benzyl ester 
• 81477-94-3 N-(diphenylmethylene)glycine tert-butyl ester 
• 870-63-3 prenyl bromide 
• 34582-32-6 N-tert-butoxycarbonyl aspartic acid tert-butyl ester 

Downstream Products

• 1407507-20-3 Di-tert-butyl (2S)-2-[(tert-butoxycarbonyl)amino]-5-(4-hydroxybenzyl)hexane-dioate 
• 1407507-30-5 Di-tert-butyl (5S)-2-(benzyloxycarbonyl)-5-[(tert-butoxycarbonyl)amino]hexane-dioate 
• 1407507-32-7 (5S)-2-(tert-Butoxycarbonyl)-5-[(tert-butoxycarbonyl)amino]-2-(4-hydroxybenzyl)-hexanedioic acid 6-tert-butyl ester 
• 1407506-27-7 di-tert-butyl (2S)-2-[(tert-butoxycarbonyl)amino]-5-{4-[2-(tosyloxy)ethoxy]benzyl}-hexanedioate 
• 1408443-30-0 di-tert-butyl (2S)-2-[(tert-butoxycarbonyl)amino]-5-{[5-(2-{[(4-methylphenyl)sulfonyl]oxy}ethoxy)pyridin-2-yl]methyl}hexanedioate 
• 1408448-97-4 4-benzyl 1,4-di-tert-butyl (1S)-6-[4-(benzyloxy)phenyl]-1-[(tert-butoxycarbonyl)amino]hexane-1,4,4-tricarboxylate 
• 1408448-99-6 (5S)-6-tert-butoxy-2-(tert-butoxycarbonyl)-5-[(tert-butoxycarbonyl)amino]-2-[2-(4-hydroxyphenyl)ethyl]-6-oxohexanoic acid 
• 1408447-37-9 di-tert-butyl (2S)-2-[(tert-butoxycarbonyl)amino]-5-[2-(4-hydroxyphenyl)ethyl]hexanedioate 
• 1408447-04-0 (2S)-2-tert-butoxycarbonylamino-5-{2-[4-(2-fluoro-ethoxy)-phenyl]-ethyl}hexanedioic acid di-tert-butyl ester 
• 1408447-80-2 (2S,5R)-2-tert.-butoxycarbonylamino-5-(4-hydroxy-benzyl)-hexanedioic acid di-tert.-butyl ester 
• 1408447-83-5 (2S,5S)-2-tert.-butoxycarbonylamino-5-(4-hydroxy-benzyl)-hexanedioic acid di-tert.-butyl ester 
• 1408449-57-9 (5S)-2-(4-aminobenzyl)-6-tert-butoxy-2-(tert-butoxycarbonyl)-5-[(tert-butoxycarbonyl)-amino]-6-oxohexanoic acid 
• 1408447-46-0 di-tert-butyl (5S)-2-(4-aminobenzyl)-5-[(tert-butoxycarbonyl)amino]hexanedioate 
• 1408449-59-1 di-tert-butyl (5S)-2-(4-{[2-(benzyloxy)ethyl]amino}benzyl)-5-[(tert-butoxycarbonyl)-amino]hexanedioate 

Relevant academic research and scientific papers

An efficient and scalable synthesis of Isodesmosine

Isodesmosine is 1,2,3,5-tetrasubstituted pyridinium-based amino acid substituted with four lysine derivatives found in elastin which is the main component of elastic fiber. Elastin plays a vital role in providing stretchy properties to tissues and body organs. Isodesmsoine is a proven to be useful biomarker for elastin degradation during the progressing stage of chronic obstructive pulmonary disease (COPD) and related diseases. The present work reported an efficient and gram-scale approach for the synthesis of Isodesmosine, starting from readily available Boc-Asp-OtBu using mild reaction conditions.

NOVEL HISTONE METHYLTRANSFERASE INHIBITORS

The present invention relates to novel compounds of formula (I) as defined herein. The compounds are inhibitors of histone methyltransferases of the seven-beta-strand family, in particular of KMT9.

Chemical synthesis of disulfide surrogate peptides by using beta-carbon dimethyl modified diaminodiacids

The replacement of disulfide bridges with metabolically stable isosteres is a promising strategy to improve the stability of disulfide-rich polypeptides towards reducing agents and isomerases. A diaminodiacid-based strategy is one of the most effective methods to construct disulfide bond mimics, but modified diaminodiacids have not been developed till now. Inspired by the fact that alkylation of disulfide bonds can regulate the activity of polypeptides, herein, we report the first example of thioether bridged diaminodiacids incorporating Cys Cβdimethyl modification, obtained by penicillamine (Pen)-based thiol alkylation. The utility of these new diaminodiacids was demonstrated by the synthesis of disulfide surrogates of oxytocin containing a short-span disulfide bond and of KIIIA with large-span disulfide bonds. This new type of synthetic bridge further extends the diaminodiacid toolbox to facilitate the study of the structure-activity relationship of disulfide-rich peptides.

Diaminodiacid bridge improves enzymatic and in vivo inhibitory activity of peptide CPI-1 against botulinum toxin serotype A

The replacement of the disulfide bridge of CPI-1, a peptide inhibitor of light chain of Botulinum toxin serotype A, with the thioether-containing and biscarba-containing diaminodiacid bridge leads to a significant decrease in the degradation by trypsin and increase in the detoxification activity in vivo, the addition of hydrophobic or positive amino acid at C-terminus of modified peptides further improves the inhibitory activity.

Improved enantioselective gram scale synthesis route to N-Fmoc-protected monofluoroethylglycine

Fluorine, as a substituent in amino acids, has found its way into peptide and protein engineering. The basis for the use of this valuable tool is the synthetic accessibility of various fluorinated amino acids as building blocks of peptides and proteins. In this context, we present a straightforward eight-step synthesis of N-Fmoc-L-monofluoroethylglycine (MfeGly) via homoserine (Hse) as intermediate and using various nucleophilic fluorination strategies.

Stereoselective Synthesis of Protected l - Allo -Enduracididine and l -Enduracididine via Asymmetric Nitroaldol Reaction

The diastereoselecetive and scalable synthesis of cyclic guanidine-containing nonproteinoginic amino acids, enduracididines, has been achieved. Both diastereomers, l - allo -enduracididine and l -enduracididine, were prepared via catalyst-controlled asymmetric nitroaldol reaction with the aldehyde precursor derived from l -aspartic acid. The cyclic guanidine of di-Cbz-protected l - allo -enduracididine was fully protected with an allyl group to suppress nucleophilic side reactions. Introduced allyl group was efficiently removed via π-allylpalladium chemistry without attaching the Cbz group on the cyclic guanidine moiety.

BIHETEROCYCLIC COMPOUND

The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter wherein R1-L- is R1—OC(O)—, or the like, R1 is hydrogen atom, optionally-substituted C1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R3 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like, the part of X, Y, and Z is X═Y—Z, X—Y═Z, or X—Y—Z, X is nitrogen atom, NR4 (R4 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.

HYPERPOLARIZED AND DEUTERIUM EXCHANGED HYPERPOLARIZED13C AND 15N-LABELED XANTHINE, ARGININE, GLUTAMINE, AND UREA PROBES

The present technology provides 13C- and 15N-labeled probes for imaging one or more mammalian cells using magnetic resonance. Thus, 13C- and 15N-labeled arginine (compound of formula I), xanthine (compounds of f

Process for preparing deuterated desmosine and derivatives thereof

There is provided a process for preparing a compound represented by the following general formula (1) or a salt thereof, which comprises exchanging one or more of an amino proton in a compound represented by the following general formula (2) or a salt thereof to deuterium, and after the exchanging, converting a deuterium-exchanged compound of the compound represented by the general formula (2) or a salt thereof into the compound represented by the general formula (1) or a salt thereof: wherein, in the general formula (1), one, or two or more of hydrogen atom may be substituted with their isotope; and in the general formula (2), each of R1 is independently hydrogen atom, tert-butyloxycarbonyl group or benzyloxycarbonyl group, and R2 is independently tert-butyl group, benzyl group, methyl group or ethyl group.