49548-40-5

Usage

Uses

N-Benzyloxycarbonylglycine Thioamide can be prepared to use as antibacterial agents.

InChI:InChI=1/C10H12N2O2S/c11-9(15)6-12-10(13)14-7-8-4-2-1-3-5-8/h1-5H,6-7H2,(H2,11,15)(H,12,13)

Upstream product

• 3589-41-1 phenylmethyl cyanomethylcarbamate 
• 18877-94-6 ethyl 2-phenylmethoxycarbonylaminoethaneimidothioate monohydrochloride 
• 501-53-1 benzyl chloroformate 
• 1138-80-3 N-(Benzyloxycarbonyl)glycine 
• 949-90-6 N-(carbobenzyloxy)glycinamide 

Downstream Products

• 140903-32-8 (Benzyloxycarbonylamino)thioacetimidsaeure-methylester-fluorsulfonat 
• 1126431-80-8 phenylmethyl ({5-(2-chloro-4-pyrimidinyl)-4-[3-methyl-5-(methyloxy)phenyl]-1,3-thiazol-2-yl}methyl)carbamate 
• 321426-45-3 C₁₃H₁₃N₃O₃S 
• 95716-01-1 Z-(gly)Thz-OH 
• 1404113-50-3 ethyl 2-((benzyloxycarbonylamino)methyl)-4-phenylthiazole-5-carboxylate 
• 1404113-49-0 benzyloxycarbonyl (4-phenylthiazol-2-yl)methylamine 
• 88621-55-0 N-(Benzyloxycarbonyl)dithioglycin-methylester 
• 610796-28-6 (R)-3-Benzyloxycarbonylamino-3-[2-(benzyloxycarbonylamino-methyl)-thiazol-4-yl]-propionic acid 
• 247233-68-7 (4-cyclohexylmethyl-thiazol-2-ylmethyl)-carbamic acid benzyl ester 

Relevant academic research and scientific papers

Azotides as Modular Peptide-Based Ligands for Asymmetric Lewis Acid Catalysis

Synthesis of azotides and evaluation of these as ligands for enantioselective Lewis acid catalysis is reported. The ligands were readily prepared from the chiral pool of amino acids and perform well in the cobalt(II)-catalyzed formation of asymmetric hete

Polythiazole linkers as functional rigid connectors: A new RGD cyclopeptide with enhanced integrin selectivity

Polythiazole amino acids clasp linear peptides to generate cyclic derivatives, however, the resulting species are not merely stapled peptides but bear a complex heterocyclic moiety displaying its intrinsic set of interactions. As a proof of concept, a bisthiazole moiety has been grafted onto an RGD sequence to deliver a new cilengitide analogue with improved integrin selectivity and remarkable in vivo antiangiogenic activity.

Core refinement toward permeable β-secretase (BACE-1) inhibitors with low hERG activity

By use of iterative design aided by predictive models for target affinity, brain permeability, and hERG activity, novel and diverse compounds based on cyclic amidine and guanidine cores were synthesized with the goal of finding BACE-1 inhibitors as a treatment for Alzheimer's disease. Since synthesis feasibility had low priority in the design of the cores, an extensive synthesis effort was needed to make the relevant compounds. Syntheses of these compounds are reported, together with physicochemical properties and structure-activity relationships based on in vitro data. Four crystal structures of diverse amidines binding in the active site are deposited and discussed. Inhibitors of BACE-1 with 3 μM to 32 nM potencies in cells are shown, together with data on in vivo brain exposure levels for four compounds. The results presented show the importance of the core structure for the profile of the final compounds.

Heterocyclic Compounds Useful as RAF Kinase Inhibitors

The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.

COMPOUNDS USEFUL AS RAF KINASE INHIBITORS

The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.

Phenolic thiazoles as novel orally-active neuroprotective agents

Novel phenolic thiazoles compounds were prepared which demonstrated potent antioxidant activity and potent in vivo neuroprotection in mitochondrial toxin models and also possess good oral bioavailability.

Synthesis of primary thioamides from nitriles and hydrogen sulfide catalyzed by anion-exchange resin

A new method has been developed for converting nitriles into primary thioamides. Treatment of various nitriles (Table 1, entries 1-12) with gaseous hydrogen sulfide in a mixture of methanol-water or ethanol-water and in the presence of anion-exchange resin (Dowex 1X8, SH- form) at room temperature and ambient pressure gave the corresponding thioamides in 25-96% yield.

Structure-based design and synthesis of a novel class of Src SH2 inhibitors

The structure-based design and synthesis of a novel class of 2,4- disubstituted thiazoles as Src SH2 inhibitors is described. Initial results are presented, including the X-ray and NMR analysis of one thiazole inhibitor bound to Lck and Src SH2.

Total synthesis of nosiheptide. Synthesis of thiazole fragments

The preparation of three new thiazole derivatives from natural products is described, as well as improvements in the synthesis of ethyl 2-aminomethyl-4-thiazolecarboxylate.

A new asymmetric synthesis of (S)-dolaphenine and its heteroaromatic congeners utilizing (+)-2-hydroxy-3-pinanone and (-)-3-hydroxy-2-caranone as chiral auxiliaries

(+)-2-hydroxy-3-pinanone ((+)-HyPN,(+)-2a) and (-)-3-hydroxy-2-caranone ((-)-2b) were respectively converted to the corresponding Schiff bases 18a and 18b with 1-(2-thiazolyl)methylamine (17). Alkylation followed by removal of the chiral auxiliaries (+)-2a and (-)-2b afforded (S)-dolaphenine (10) as an optically pure form. The method was applied to the asymmetric synthesis of the dolaphenine analogs 27a-d.