57699-50-0

Upstream product

• 870-46-2 t-butoxycarbonylhydrazine 
• 104-88-1 4-chlorobenzaldehyde 
• 119-61-9 benzophenone 

Downstream Products

• 57699-57-7 N-(tert-butoxycarbonyl)-N'-(4-chlorobenzyl)hydrazine 
• 1422157-62-7 N′-[chloro-(4-chlorophenyl)methylene]-tert-butylcarbazate 
• 1711-61-1 5-(4-chlorophenyl)-3H-[1,3,4]oxadiazol-2-one 
• 57699-65-7 tert-Butoxycarbonyl-(α-aza-4-chlorphenylalanin)-ethylester 
• 57699-71-5 1-Carbamoyl-1-(4-chlorbenzyl)-2-tert-butoxycarbonylhydrazin 

Relevant academic research and scientific papers

The continuous-flow synthesis of carbazate hydrazones using a simplified computer-vision controlled liquid–liquid extraction system

A computer-vision controlled liquid–liquid extraction system was used in the continuous-flow synthesis of a series of carbazate hydrazones. The system uses open-source software components (Python, OpenCV) and is simpler and potentially more economical, in terms of hardware, than one we have described previously.

Synthesis and biological evaluation of Hydrazone derivatives as antifungal agents

Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-Toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C.Tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae) and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs) of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a) and tert-butyl-(2Z)-2-(3,4,5-Trihydroxybenzylidine)hydrazine carboxylate (7b) showed the most promising MIC values in the range of 16-32 μg/mL and 8-16 μg/mL, respectively. The compounds' action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents.

Synthesis of 5-aryl-3H-[1,3,4]oxadiazol-2-ones from N′-(chloro-aryl- methylene)-tert-butylcarbazates using basic alumina as an efficient and recyclable surface under solvent-free condition

The synthesis of biologically important 5-aryl-3H-[1,3,4]oxadiazol-2-ones has been carried out by heating the easily synthesized N′-(chloro-aryl- methylene)-tert-butylcarbazates on basic alumina surface under solvent-free condition. The dual characteristic of basic alumina as a solid support as well as a nucleophile is successfully exploited in these reactions. The method provides special attributions such as reduced reaction times, easier work-up procedures, and good to excellent yields as well as increased purity of products and most importantly environmentally friendly protocols. The basic alumina is easily recovered and utilized for further reactions several times without serious loss of activity.

Phase-transfer catalytic aza-Michael addition of tert-butyl benzyloxycarbamate to electron-deficient olefins

A highly efficient phase-transfer catalytic aza-Michael addition of tert-butyl benzyloxycarbamate to a wide range of electron-deficient olefins is presented (90-99%). The Royal Society of Chemistry.

Design of selective peptidomimetic agonists for the human orphan receptor BRS-3

New tool substances may help to unravel the physiological role of the human orphan receptor BRS-3 and its possible use as a drug target for the treatment of obesity and cancer. In continuation of our work on BRS-3, the solid- and solution-phase synthesis of a library of low molecular weight peptidomimetic agonists based on the recently developed short peptide agonist 4 is described. Functional potencies of the compounds were determined measuring calcium mobilization in a fluorometric imaging plate reader (FLIPR) assay. Focusing on the N-terminus, the D-Phe-Gln moiety of 4 was modified in a combinatorial SAR-oriented medicinal chemistry approach. With the incorporation of N-arylated glycine and alanine building blocks azaglycine, piperazine, or piperidine and the synthesis of semicarbazides and semicarbazones, a number of highly potent and selective compounds with a reduced number of peptide bonds were obtained, which also should have enhanced metabolic stability.

NON-PEPTIDIC BRS-3 AGONISTS

The invention relates to novel compounds having a selective BRS-3 agonistic action and corresponding to general formula (I) wherein A1, A2, A3, R1, R2, R3, Ar1, Ar2, Ar3, m and n have the designations cited in the description. The invention also relates to pharmaceuticals containing said compounds and to methods for producing compounds of formula (I).

Sodium cyanoborohydride reduction of (benzyloxycarbonyl)- and (tert-butoxycarbonyl)hydrazones

(Benzyloxycarbonyl)- and (tert-butoxycarbonyl)hydrazones are easily reduced by sodium cyanoborohydride in acidic medium. The method is an alternative to catalytic hydrogenation and allows ready access to both N-benzyloxycarbonyl and N-tert-butoxycarbonyl