66012-26-8

Upstream product

• 3417-91-2 L-tyrosine methyl ester HCl 
• 1080-06-4 L-Tyr-OMe 
• 1138-80-3 N-(Benzyloxycarbonyl)glycine 
• 1330059-26-1 N-benzyloxycarbonylglycine 9-fluorenylmethyl thioester 
• 16707-70-3 2-(((benzyloxy)carbonyl)amino)ethanethioic S-acid 
• 35264-84-7 ZGly, triethylammonium salt 
• 1080-06-4 L-Tyr-OCH₃ 
• 67-56-1 methanol 
• 19790-44-4 Cbz-Gly-Tyr-NH₂ 
• 80681-01-2 [2-Oxo-2-(2-thioxo-thiazolidin-3-yl)-ethyl]-carbamic acid benzyl ester 

Downstream Products

• 193274-60-1 (S)-3-(4-Methoxymethoxy-benzyl)-piperazine-2,5-dione 
• 934840-98-9 C₂₈H₃₀N₄O₆ 
• 193625-90-0 Z-Gly-Tyr-Gly-Gly-Pro-Phe-Pro-OBz 
• 193625-89-7 H-Gly-Tyr-Gly-Gly-Pro-Phe-Pro-OH 
• 184713-88-0 Z-Gly-Tyr-Gly-GlyOEt 
• 122411-87-4 {2-[(S)-2-(2-Benzyloxycarbonylamino-acetylamino)-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetic acid 
• 7801-35-6 Cbz-G-Y-OH 

Relevant academic research and scientific papers

PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITORS AS diAGNOSTIC AND RAdiONUCLIDE THERAPEUTIC AGENTS

The present disclosure relates to compounds according to Formula I. These compounds display very good binding affinities to the PSMA binding sites. They comprise a radioactive isotope or a chelating moiety that can be labeled with a radioactive metal such as [68Ga]or [177Lu]. The present disclosure also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or a complex thereof, or a pharmaceutically acceptable salt thereof.

One-step C-terminal deprotection and activation of peptides with peptide amidase from stenotrophomonas maltophilia in neat organic solvent

Chemoenzymatic peptide synthesis is a rapidly developing technology for cost effective peptide production on a large scale. As an alternative to the traditional C→N strategy, which employs expensive N-protected building blocks in each step, we have investigated an N→C extension route that is based on activation of a peptide C-terminal amide protecting group to the corresponding methyl ester. We found that this conversion is efficiently catalysed by Stenotrophomonas maltophilia peptide amidase in neat organic media. The system excludes the possibility of internal peptide cleavage as the enzyme lacks intrinsic protease activity. The produced peptide methyl ester was used for peptide chain extension in a kinetically controlled reaction by a thermostable protease.

Processes for forming amide bonds and compositions related thereto

The disclosure relates to methods for producing amide bonds and reagents related thereto. In some embodiments, the disclosure relates to methods of producing an amide comprising mixing an O-silylated thionoester and an amine under conditions such that an amide is formed. In another embodiment, the disclosure relates to mixing a thiolacid, a silylating agent, and an amine under conditions such that an amide is formed.

In situ carboxyl activation using a silatropic switch: A new approach to amide and peptide constructions

The novel reactivity of O-silylthionoesters with amine nucleophiles to generate oxoamides (rather than thioamides) is described. A straightforward first-generation trimethylsilylation protocol using bistrimethylsilylacetamide (BSA) combined with the unique reactivity of the O-silylthionoesters toward 1° and 2° amines to generate oxoamides provides the simplest means of activating a thiol acid for peptide bond formation at neutral pH. Excellent stereoretention is observed.

Application of an organophosphorus reagent depbt for synthesis of cycloheptapeptide

A cycloheptapeptide cyclo(Gly-Tyr-Gly-Gly-Pro-Phe-Pro), which was isolated and identified from one kind of Chinese medicinal herbs, was chosen as a model cyclopeptide, to evaluate an organophosphorus reagent, 3-(diethyloxyphosphoryloxy)-1,2,3-benzotriazin

Total syntheses of naturally occurring bis(methylthio)silvatin and its three stereoisomers

Total syntheses of naturally occurring bis(methylthio)silvatin and its three stereoisomers were achieved from l,4-dimethyl-3-(p-hydroxy)benzyl-2,5-piperazinedione. The configurational structures of the four stereoisomers, thus obtained, were definitely determined by the comparisons of their mps, specific rotations and NMR spectra.

A low-epimerizing peptide coupling reagent based on the rearrangement of a carboxylic-sulfonic mixed anhydride

A series of peptides has been prepared using an o-hydroxybenzenesulfonyl chloride as the condensation reagent. Experimentally, the coupling is a one pot two-steps reaction: formation and aminolysis of a substituted aryl ester. The first step occurs by an

Peptide Synthesis with Benzo- and Naphthosultones

6-Nitro- and 6,8-dinitronaphth-1,2-oxathiole S,S-dioxides (7b and 7c) have been prepared from the parent naphthosultone 7a and compared with 5-nitrobenz-3H-1,2-oxathiole S,S-dioxide (1b) as coupling reagents for peptide synthesis.Nucleophilic attack of a carboxylate salt on these strained five-membered sultones leads to activated esters 3 and 9 which rapidly react with amines (except in the case of 9c).The rate constant for the formation of ester 9b is higher than that of 3b.Amides or peptides are formed in slightly better yields with the naphthosultone 7b than with the benzosultone 1b.The naphthosultones are also preferred over the benzosultones from the point of view of amount of 5(4H)-oxazolone formation from N-benzoyl amino acids and the degree of racemization.However the rate of alkaline hydrolysis of 7b is slower than that of 1b.All these results may be rationalized by a better intramolecular acyl transfer reaction in the more rigid mixed anhydride intermediate 8b.There is no dependence on in the rate equation for aminolysis of esters 3b and 9b by benzylamine in THF, acetonitrile, or DMF and the aminolysis is probably anchimerically assisted by a neighbouring S=O group.Esters 3b are more selective acylating agents for primary amino groups in the presence of secondary ones than esters 9b and this observation is exploited in a synthesis of maytenine by selective acylation of spermidine.

3-AMINOACYL-TETRAHYDROTHIAZOLE-2-THIONE AS AN ACTIVE AMIDE FOR PEPTIDE SYNTHESIS (I)

3-Aminoacyl-tetrahydrothiazole-2-thione can be used as an active amide for peptide synthesis.A series of peptides have been synthesized with satisfactory yields by this methods.