213475-74-2

Upstream product

• 213475-73-1 tert-butyl (1,3-diazidopropan-2-yl)carbamate 
• 213475-67-3 [2-benzyloxycarbonylamino-1-(benzyloxycarbonylaminomethyl)ethyl]carbamic acid tert-butyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 125414-41-7 N-Boc-serinol 
• 213475-70-8 methanesulfonic acid 2-tert-butoxycarbonylamino-3-methanesulfonyloxypropylester 
• 2766-43-0 N-tert-butyloxycarbonyl-L-serine methyl ester 

Downstream Products

• 1448674-43-8 tert-butyl {2-[4-(benzyloxy)phenyl]-1,4,5,6-tetrahydropyrimidin-5-yl}carbamate 
• 1448674-44-9 tert-butyl 2-[4-(benzyloxy)phenyl]-5-[(tert-butoxycarbonyl)amino]-5,6-dihydropyrimidine-1(4H)-carboxylate 
• 1448674-45-0 tert-butyl 5-[(tert-butoxycarbonyl)amino]-2-(4-hydroxyphenyl)-5,6-dihydropyrimidine-1(4H)-carboxylate 
• 1122410-63-2 {1-aminomethyl-2-[4-(4-methoxybenzyloxy)-quinolin-2-ylamino]ethyl}carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

GUANIDINE-MODIFIED C-TERMINUS VANCOMYCIN COMPOUNDS, COMPOSITIONS AND METHODS

A series of vancomycin C-terminus guanidine modifications are disclosed that improve antimicrobial activity, enhance the durability of antimicrobial action against selection or induction of resistance, and provide two synergistic mechanisms of action inde

Serine- and threonine-derived diamine equivalents for site-specific incorporation of platinum centers in peptides, and the anticancer potential of these conjugates

A modular strategy that allows introduction of one or more reactive platinum units at chosen locations along a peptide sequence is presented. This makes use of diazides generated from serine and threonine as diamine equivalents which can be conjugated to the peptide under standard coupling conditions. Reduction of these diazides using Pd/C and H2 followed by platination affords the final products in good yields. Following this, we prepared a new class of peptide-platinum conjugates and carried out preliminary cytotoxicity evaluation and DNA interaction studies. Inclusion of lysine residues in the sequence was found to improve DNA interaction and anticancer activities compared to analogous conjugates with hydrophobic side chains.

2-[2-Substituted-3-(3,4-dichlorobenzylamino)propylamino]-1H-quinolin-4-ones as Staphylococcus aureus methionyl-tRNA synthetase inhibitors

New analogues of 2-[2-substituted-3-(3,4-dichlorobenzylamino)propylamino]quinolin-4-ones, 26a, 26b, 31a-e, 34, 35, 38 and 40, have been synthesized and evaluated against Staphylococcus aureus methionyl-tRNA synthetase. All of the synthesized compounds were less active than the reference compound 2. The compounds were also screened against various strains of S. aureus and Enterococci for their antibacterial activities. Among the compounds, 26b, 31c and 31e displayed significant inhibitory properties against various strains of Enterococci compared to compound 2.

Development of a chemoenzymatic strategy for the synthesis of optically active and orthogonally protected polyamines

The chemical preparation and stereoselective enzymatic desymmetrization of a series of prochiral 2-substituted-1,3-propanediamines have been carried out using Pseudomonas cepacia lipase as biocatalyst. Syntheses of novel optically active orthogonally protected di- or triamines have been achieved for the first time with different grade of enantiodiscrimination depending on the C-2 substitution of the propane-1,3-diamine fragment. Final monoselective deprotection reactions of (S)-3-allyl-2-tert-butyl-1-(9-fluorenylmethyl)propane-1,2,3-triyltriscarbamate have allowed us to obtain a panel of novel enantiomerically enriched disubstituted triamines, compounds of difficult access by conventional synthetic methods.

Convenient and simplified approaches to w-monoprotected triaminopropane derivatives: Key intermediates for bifunctional chelating agent synthesis

High yields of selectively Ar-protected-1,2,3-triaminopropanes (1,3 or 1,2 functionalized diamines) were obtained in 6 or 4 steps from diamino alcohols or aminodiols, respectively. These two multi-step procedures involve protection of the amino group, substitution of the hydroxy group by an azido group and selective reduction. The conditions for the first procedure allow the preparation of various Af2-monoprotected-l,2,3-triaminopropanes 6a, 6b, but the second one is more convenient for obtaining N1-Boc-1,2,3-triaminopropane 6'. These two simplified procedures, which provide functionalized 1,2 or 1,3 diamines easily and with good overall yields, could be useful for the synthesis of : bifunctional chelating agents.