4792-54-5

Upstream product

• 91301-06-3 2-cyano-2-hydroxy-propionic acid ethyl ester 
• 100-63-0 phenylhydrazine 
• 100-34-5 benzene diazonium chloride 
• 609-08-5 Diethyl methylmalonate 
• 617-35-6 2-oxo-propionic acid ethyl ester 
• 2684-02-8 benzenediazonium 
• 27772-62-9 ethyl 2-formylpropionate 
• 64-17-5 ethanol 
• 59-88-1 phenylhydrazine hydrochloride 
• 36966-84-4 Nitrosophenylamine 
• 62-53-3 aniline 
• 7664-93-9 sulfuric acid 
• 5330-70-1 pyruvic acid phenylhydrazone 

Downstream Products

• 1477-50-5 Indole-2-carboxylic acid 
• 3770-50-1 2-carbethoxyindole 
• 5330-70-1 pyruvic acid phenylhydrazone 
• 220437-87-6 5-ethoxycarbonyl-5-methyl-2-phenyl<1,2,4>triazolidine-3-thione 
• 19005-93-7 1H-indol-2-ylcarboxaldehyde 
• 56809-86-0 1-methyl-1H-indole-2-carbohydrazide 
• 1488427-09-3 N-{{5-fluoro-2-[5-(isopropylthio)-4-phenyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indol-3-yl}methyl}-3-morpholinopropan-1-amine 
• 1488427-06-0 N-{{2-[5-(isopropylthio)-4-phenyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indol-3-yl}methyl}-2-morpholinoethan-1-amine 
• 1488427-08-2 N-{{2-[5-(isopropylthio)-4-phenyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indol-3-yl}methyl}-3-morpholinopropan-1-amine 
• 1488427-18-4 2-[5-(isopropylthio)-4-phenyl-4H-1,2,4-triazol-3-yl]-1-methyl-3-[(4-methylpiperidin-1-yl)methyl]-1H-indole 

Relevant academic research and scientific papers

Method for preparing perindopril despinner and intermediate thereof

The invention discloses a method for preparing perindopril despinner and an intermediate thereof. The method comprises the following steps: halogenating N-propionyl indole-2-carboxylic acid under theaction of a halogenation reagent so as to obtain a halogenation product, and further carrying out amine substitution and catalytic hydrogenation reduction on the obtained halogenation product, therebyobtaining the perindopril despinner. Compared with the prior art, the method is cheap and easy in reaction raw material, has a total yield as high as 64%, is high in product purity and is applicableto industrial production.

Substituted indole - 2 - formic acid (by machine translation)

This invention relates to a substituted indole - 2 - carboxylic acid synthesis method, is to replace the phenyl hydrazine hydrochloride or arylhydrazines as raw materials, through with pyruvic acid ethyl ester cheng zong, Fischer indole synthesis by reaction of substituted indole - 2 - carboxylic acid ethyl ester, hydrolysis to obtain the substituted - 2 - carboxylic acid. Product purity is greater than 97%, the reaction yield is 64%. Synthesis method of the invention with non-harsh conditions, the operation is simple, and environmental friendliness, it has certain economic benefits. It is a kind of raw materials are easy, simple operation, three wastes, high yield of indole - 2 - carboxylic acid synthesis method. (by machine translation)

Sulfamic acid as a green, reusable catalyst for stepwise, tandem & one-pot solvent-free synthesis of pyrazole derivatives

Sulfamic acid (SA) is a bi-functional, cost-effective and reusable green catalyst for the synthesis of 4-(pyrazol-4-yl)methylenepyrazol-5(4H)-one derivatives by one-pot, three-component condensation of pyrazol-4-carbaxaldehydes, β-ketoesters and phenyl hydrazine (Route-I). In addition to this method, another simple condensation of pyrazol-4-carbaxaldehydes with pyrazolone in the presence of SA under the solvent-free condition in good yield is reported. The merits of these protocols are mild conditions, non-aqueous workup, high yields, easy availability of the catalyst, no chromatographic separation and inexpensive solid acid catalyst. Furthermore, SA could be recycled and reused for five times without losing its catalytic activity.

Rh(II)-catalyzed intramolecular annulation of N-sulfonyl 1,2,3-triazoles with indole derivatives: A new method for synthesis pyranoindoles

A direct and highly stereoselective approach for the synthesis of Z-alkenyl-pyranoindoles had been developed by utilizing Rh(II)-catalyzed intramolecular cyclization of N-sulfonyl-1,2,3-triazoles with indole derivatives. A variety of pyranoindoles were obtained in 44-93% yields. Moreover, a more convenient synthesis of pyranoindoles starting from terminal alkyne was realized via a Cu-Rh sequentially catalyzed one-pot cascade reaction.

Synthesis of novel 5-[(1,2,3-triazol-4-yl)methyl]-1-methyl-3H-pyridazino[4,5-b]indol-4-one derivatives by click reaction and exploration of their anticancer activity

A series of pyridazino[4,5-b]indole derivatives containing alkyl-, benzyl- and phenacyl-substituted 1,2,3-triazolylmethyl units was synthesized using click chemistry approach. All 30 compounds of the series were screened in vitro against four cancer cell lines, viz. breast cancer cells MDA-MB-231 and MCF 7, human primary glioblastoma U-87 and human neuroblastoma IMR-32 cell lines. Most of the compounds exhibited potent cancer cell growth inhibition activity at very low micromolar concentrations. The IC50 value of compounds 7v and 7x against human neuroblastoma IMR-32 cell line is 0.07 and 0.04 μM, respectively. Among the tested compounds, ten compounds showed IC50 value less than 1 μM against MDA-MB-231 cells, whereas against IMR-32 cells, nine compounds and, against U-87 cells, six compounds showed similar inhibition activity. Further, these molecules exhibited prominent binding affinity and docking scores in the molecular simulation study with the target enzyme PI3 kinase. Graphical Abstract: This paper illustrates the synthesis of new fused indole-pyridazinone derivatives containing substituted 1,2,3-triazoles via click chemistry approach. Most of the compounds exhibited potent cancer cell growth inhibition activity at very low micromolar concentrations. [Figure not available: see fulltext.]

A new class of efficient 4-[(nitro substituted-phenyl)-hydrazonomethyl]-1-phenyl-1H-pyrazole-3-carboxylate derived colorimetric chemosensor for selective sensing of fluoride and other biologically important anions

A new class of efficient colorimetric chemosensors derived from 4-[(nitro substituted-phenyl)-hydrazonomethyl]-1-phenyl-1H-pyrazole-3-carboxylate have been synthesized and characterized. The synthesized receptors exhibit instant color change from yellow t

ZnO nanoparticles as reusable heterogeneous catalyst for efficient one pot three component synthesis of imidazo-fused polyheterocycles

An efficient, simple, environmentally benign synthetic protocol is developed for synthesis of biologically and medicinally relevant pyrazole coupled imidazo[1,2-a]pyridine derivatives via three component reaction of alkyl-4-formyl-1-phenyl-1H-pyrazole-3-c

Indole-3-carbinol and 1,3,4-oxadiazole hybrids: Synthesis and study of anti-proliferative and anti-microbial activity

In the present study, molecular hybrids of indole-3-carbinol and 1,3,4-oxadiazole-2-thiols have been designed and synthesized. The thiol analogues consisted of diversely substituted benzyl and alkyl groups with different electronic properties. The structures of all the newly synthesized scaffolds and target compounds were ascertained using 1H NMR, 13C NMR, mass spectrometry, and elemental analyses. All the final compounds were screened in vitro for their anti-proliferative and anti-microbial activity. Three compounds showed excellent anti-proliferative activity with more than 70% cell growth inhibition against three cancer cell lines, HepG2 (human liver hepatocellular carcinoma), HeLa (human cervix carcinoma), and MCF-7 (human breast carcinoma). In the anti-microbial studies, compounds with electron-withdrawing fluoro or nitro substituent displayed appreciable activity similar to that of standard drugs. Also, the final compounds are non-toxic to non-cancerous Vero cell line.

Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition

In our pursuit to develop new potential anticancer leads, we designed a combination of structural units of indole and substituted triazole; and a library of 1-{1-methyl-2-[4-phenyl-5-(propan-2-ylsulfanyl)-4H-1,2,4-triazol-3- yl]-1H-indol-3-yl}methanamine derivatives was synthesized and characterized. Cytotoxic evaluations of these molecules over a panel of three human cancer cell lines were carried out. Few molecules exhibited potent growth inhibitory action against the treated cancer cell lines at lower micro molar concentration. An in vitro assay investigation of these active compounds using recombinant human SIRT1 enzyme showed that one of the compounds (IT-14) inhibited the deacetylation activity of the enzyme. The in vivo study of IT-14 exemplified its promising action by reducing the prostate weight to the body weight ratio in prostate hyperplasia animal models. A remarkable decrease in the disruption of histoarchitecture of the prostate tissues isolated from IT-14 treated animal compared to that of the positive control was observed. The molecular interactions with SIRT1 enzyme were also supported by molecular docking simulations. Hence this compound can act as a lead molecule to treat prostatic hyperplasia.

Reaction of Lawesson's reagent with ester hydrazones: Synthesis of novel 3-thioxo-1,2,3-diazaphospholine derivatives

The reaction of ester hydrazones with Lawesson's reagent leads to a variety of new 3-thioxo-1,2,3-diazaphospholine derivatives. The reaction shows relative regioselectivity and gives in some cases a mixture of two diastereoisomers. The electronic and steric factors influencing the regioselectivity of the reaction are discussed.