Tag: 278.1334

Synthesis and characterization of specified impurities of aceclofenac was written by Somashekar, P. L.;Pai, P. N. Sanjay;Rao, Gopalkrishna. And the article was included in Chemical Science Transactions in 2013.Computed Properties of C14H9Cl2NO This article mentions the following:

The present study aimed at synthesizing the process related potential impurities of aceclofenac. Aceclofenac is an orally administered benzeneacetic acid derivative with effects on a variety of inflammatory mediators. Process-related impurities of aceclofenac listed in the British Pharmacopoeia have been synthesized by modified methods and characterized by FT IR, MS and ¹H NMR data. Impurity A [i.e., [2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid (diclofenac)] was synthesized by acid hydrolysis of diclofenac sodium. Impurity B [i.e., Me [2-[(2,6-dichlorophenyl)amino]phenyl]acetate (Me ester of diclofenac)], impurity C [i.e., Et [2-[(2,6-dichlorophenyl)amino]phenyl]acetate (Et ester of diclofenac)], impurity D [i.e., Me [[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate (Me ester of aceclofenac)], impurity E [i.e., Et [[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate (Et ester of aceclofenac)] were synthesized by simple and convenient direct methylation and ethylation of diclofenac and aceclofenac resp. instead of a tedious esterification process. Impurity F [i.e., benzyl [[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate (benzyl ester of aceclofenac)] was synthesized by a condensation reaction of diclofenac sodium with benzyl bromoacetate. Impurity I [i.e., 1-(2,6-dichlorophenyl)-1,3-dihydro-2H-indol-2-one] was synthesized by an acid mediated cyclization of diclofenac. The present study has provided an efficient method for synthesis of process related aceclofenac impurities. The synthesis of the target compounds was achieved using 2-[(2,6-dichlorophenyl)amino]benzeneacetic acid carboxymethyl ester (Aceclofenac) also as a starting material. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Computed Properties of C14H9Cl2NO).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Computed Properties of C14H9Cl2NO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In vitro cytotoxicity evaluation of diversely substituted N-aryl-2-oxindoles was written by Manvar, Atul;Bavishi, Abhay;Loriya, Rajesh;Jaggi, Manu;Shah, Anamik. And the article was included in Medicinal Chemistry Research in 2013.Reference of 15362-40-0 This article mentions the following:

In continuation with our previous work, structurally diverse 2-indolinones bearing 2,6-dichloroaryl fragment at N¹ and (hetero)aryl benzylidene at C³ were evaluated for their antitumor activity on a panel of cancer cell lines such as MCF-7 (breast), MiapaCa2 (pancreas), KB (oral), HuTu80 (stomach), L132 (lung), B16F10 (melanoma), and Molt4 (leukemia) from various human organs. Among the screened compound library, mols. 4e,4k, and 4r have shown excellent cytotoxicity on a stomach cancer cell line. Moreover, a significant number of compounds have also shown promising cytotoxicity on pancreas and oral cancer cell lines. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Reference of 15362-40-0).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Reference of 15362-40-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Fate of pharmaceuticals and their transformation products in integrated membrane systems for wastewater reclamation was written by Mamo, J.;Garcia-Galan, M. J.;Stefani, M.;Rodriguez-Mozaz, S.;Barcelo, D.;Monclus, H.;Rodriguez-Roda, I.;Comas, J.. And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) in 2018.Reference of 15362-40-0 This article mentions the following:

The removal of pharmaceuticals (PhACs) from urban wastewater by membrane bioreactors (MBRs) followed by reverse osmosis (RO) or nanofiltration (NF) membranes has been frequently addressed in the literature. However, data regarding the removal of their main human metabolites and transformation products (TPs) is still scarce. Here, the presence of 13 PhACs and 20 of their metabolites and TPs was monitored during 2 consecutive years in the different treatment steps of urban raw wastewater (sewer, primary treatment, MBR and RO/NF). Rejection of the selected contaminants when using low pressure NF membranes (NF-90) or RO membranes (ESPA 2) after the MBR step was also studied. The analgesic acetaminophen, which was found at the highest concentrations in the sewer and influent samples (18-74 渭g/L) over the 2 exptl. periods, was fully eliminated during MBR treatment. Those PhACs that were only partially removed after the MBR, were almost completely removed (>99%) by the RO membrane working under different process conditions. At a similar average permeate fluxes (18 L/m²-h), the NF membrane showed high removal efficiencies (>90%) for all of the PhACs and their metabolites, though lower than those achieved by the RO membrane. When the flux of the NF90 membrane was increased to 30 L/m²-h (while still operating at a feed pressure lower than the RO membrane at 18 L/m²-h) the performance of the membrane increased, achieving 98% rejection of PhACs. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Reference of 15362-40-0).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Reference of 15362-40-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and antiproliferative activity of some novel amides of flufenamic acid and diclofenac was written by Elsaman, Tilal;Aldeeb, Omar A. A.;Aboul-Fadl, Tarek;Al-Dhfyan, Abdullah. And the article was included in Pharma Chemica in 2016.Synthetic Route of C14H9Cl2NO This article mentions the following:

Coupling of the non-steroidal anti-inflammatory drugs (NSAIDs), flufenamic acid 2 and diclofenac 5 with the appropriate amino acid ester 6, using dicyclohexylcarbdiimide (DCC), afforded amides 7-17, resp. The structures of the newly synthesized amides 7-17 were confirmed on the basis of their spectral data and X-ray single crystal anal. All the synthesized compounds have been screened for anti-proliferative activity against A549 lung adenocarcinoma and HT-29 colon cancer cells. Compound 17 showed a good anti-proliferative activity IC50 = 25.82 渭M compared with the chemotherapeutic agent 5-fluorouracil IC50 = 18 渭M. Furthermore, compound 8 was more potent than the reference drug with IC50 = 15.4渭M and cell cycle blockade activity at G0 and S-phase. Compounds 11, 12, 13 and 17 were more potent than the reference drug dichlorofluorescein diacetate (DCF) IC50 = 17.81 渭M, while the IC50 for these compound ranges from 6.46-13.99 渭M. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Synthetic Route of C14H9Cl2NO).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Synthetic Route of C14H9Cl2NO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Characterization of a reference standard for qualification of differential scanning calorimetry intended for purity determination in certification of pharmaceutical reference standards was written by Leontiev, D. A.;Volovyk, N. V.;Bevz, O. V.;Vashchenko, O. V.;Gryzodub, O. I.. And the article was included in Journal of Pharmaceutical Sciences and Research in 2018.Recommanded Product: 1-(2,6-Dichlorophenyl)-2-indolinone This article mentions the following:

To select and characterize a reference standard for equipment qualification suitable for performance verification in the certification of pharmaceutical reference standards by differential scanning calorimetry (DSC) based on the metrol. criteria of the State Pharmacopoeia of Ukraine. The purity analyses were performed in accordance with a standard procedure by DSC. For the selected candidate, the results of purity determination were compared with those obtained by gas chromatog. The metrol. criteria for results of purity determination in the certification of pharmaceutical reference standards by DSC used as an alternative method were formulated. A candidate material of cholesterol for performance verification of DSC met the established requirements. For cholesterol, the characteristics of purity, m.p. and enthalpy of fusion were certified simultaneously. The further study of intra- and inter-laboratory variation of the results is required to characterize the uncertainty of the purity determination A candidate material of cholesterol can be used as a reference standard for equipment qualification for purity determination by DSC for characterization of pharmaceutical reference standards In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Recommanded Product: 1-(2,6-Dichlorophenyl)-2-indolinone).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Recommanded Product: 1-(2,6-Dichlorophenyl)-2-indolinone

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and characterization of specified impurities of aceclofenac was written by Somashekar, P. L.;Pai, P. N. Sanjay;Rao, Gopalkrishna. And the article was included in Chemical Science Transactions in 2013.Computed Properties of C14H9Cl2NO This article mentions the following:

The present study aimed at synthesizing the process related potential impurities of aceclofenac. Aceclofenac is an orally administered benzeneacetic acid derivative with effects on a variety of inflammatory mediators. Process-related impurities of aceclofenac listed in the British Pharmacopoeia have been synthesized by modified methods and characterized by FT IR, MS and ¹H NMR data. Impurity A [i.e., [2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid (diclofenac)] was synthesized by acid hydrolysis of diclofenac sodium. Impurity B [i.e., Me [2-[(2,6-dichlorophenyl)amino]phenyl]acetate (Me ester of diclofenac)], impurity C [i.e., Et [2-[(2,6-dichlorophenyl)amino]phenyl]acetate (Et ester of diclofenac)], impurity D [i.e., Me [[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate (Me ester of aceclofenac)], impurity E [i.e., Et [[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate (Et ester of aceclofenac)] were synthesized by simple and convenient direct methylation and ethylation of diclofenac and aceclofenac resp. instead of a tedious esterification process. Impurity F [i.e., benzyl [[[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]acetate (benzyl ester of aceclofenac)] was synthesized by a condensation reaction of diclofenac sodium with benzyl bromoacetate. Impurity I [i.e., 1-(2,6-dichlorophenyl)-1,3-dihydro-2H-indol-2-one] was synthesized by an acid mediated cyclization of diclofenac. The present study has provided an efficient method for synthesis of process related aceclofenac impurities. The synthesis of the target compounds was achieved using 2-[(2,6-dichlorophenyl)amino]benzeneacetic acid carboxymethyl ester (Aceclofenac) also as a starting material. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Computed Properties of C14H9Cl2NO).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Computed Properties of C14H9Cl2NO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In vitro cytotoxicity evaluation of diversely substituted N-aryl-2-oxindoles was written by Manvar, Atul;Bavishi, Abhay;Loriya, Rajesh;Jaggi, Manu;Shah, Anamik. And the article was included in Medicinal Chemistry Research in 2013.Reference of 15362-40-0 This article mentions the following:

In continuation with our previous work, structurally diverse 2-indolinones bearing 2,6-dichloroaryl fragment at N¹ and (hetero)aryl benzylidene at C³ were evaluated for their antitumor activity on a panel of cancer cell lines such as MCF-7 (breast), MiapaCa2 (pancreas), KB (oral), HuTu80 (stomach), L132 (lung), B16F10 (melanoma), and Molt4 (leukemia) from various human organs. Among the screened compound library, mols. 4e,4k, and 4r have shown excellent cytotoxicity on a stomach cancer cell line. Moreover, a significant number of compounds have also shown promising cytotoxicity on pancreas and oral cancer cell lines. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Reference of 15362-40-0).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Reference of 15362-40-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Fate of pharmaceuticals and their transformation products in integrated membrane systems for wastewater reclamation was written by Mamo, J.;Garcia-Galan, M. J.;Stefani, M.;Rodriguez-Mozaz, S.;Barcelo, D.;Monclus, H.;Rodriguez-Roda, I.;Comas, J.. And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) in 2018.Reference of 15362-40-0 This article mentions the following:

The removal of pharmaceuticals (PhACs) from urban wastewater by membrane bioreactors (MBRs) followed by reverse osmosis (RO) or nanofiltration (NF) membranes has been frequently addressed in the literature. However, data regarding the removal of their main human metabolites and transformation products (TPs) is still scarce. Here, the presence of 13 PhACs and 20 of their metabolites and TPs was monitored during 2 consecutive years in the different treatment steps of urban raw wastewater (sewer, primary treatment, MBR and RO/NF). Rejection of the selected contaminants when using low pressure NF membranes (NF-90) or RO membranes (ESPA 2) after the MBR step was also studied. The analgesic acetaminophen, which was found at the highest concentrations in the sewer and influent samples (18-74 μg/L) over the 2 exptl. periods, was fully eliminated during MBR treatment. Those PhACs that were only partially removed after the MBR, were almost completely removed (>99%) by the RO membrane working under different process conditions. At a similar average permeate fluxes (18 L/m²-h), the NF membrane showed high removal efficiencies (>90%) for all of the PhACs and their metabolites, though lower than those achieved by the RO membrane. When the flux of the NF90 membrane was increased to 30 L/m²-h (while still operating at a feed pressure lower than the RO membrane at 18 L/m²-h) the performance of the membrane increased, achieving 98% rejection of PhACs. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Reference of 15362-40-0).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Reference of 15362-40-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Synthesis and antiproliferative activity of some novel amides of flufenamic acid and diclofenac was written by Elsaman, Tilal;Aldeeb, Omar A. A.;Aboul-Fadl, Tarek;Al-Dhfyan, Abdullah. And the article was included in Pharma Chemica in 2016.Synthetic Route of C14H9Cl2NO This article mentions the following:

Coupling of the non-steroidal anti-inflammatory drugs (NSAIDs), flufenamic acid 2 and diclofenac 5 with the appropriate amino acid ester 6, using dicyclohexylcarbdiimide (DCC), afforded amides 7-17, resp. The structures of the newly synthesized amides 7-17 were confirmed on the basis of their spectral data and X-ray single crystal anal. All the synthesized compounds have been screened for anti-proliferative activity against A549 lung adenocarcinoma and HT-29 colon cancer cells. Compound 17 showed a good anti-proliferative activity IC50 = 25.82 μM compared with the chemotherapeutic agent 5-fluorouracil IC50 = 18 μM. Furthermore, compound 8 was more potent than the reference drug with IC50 = 15.4μM and cell cycle blockade activity at G0 and S-phase. Compounds 11, 12, 13 and 17 were more potent than the reference drug dichlorofluorescein diacetate (DCF) IC50 = 17.81 μM, while the IC50 for these compound ranges from 6.46-13.99 μM. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0Synthetic Route of C14H9Cl2NO).

1-(2,6-Dichlorophenyl)-2-indolinone (cas: 15362-40-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Synthetic Route of C14H9Cl2NO

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles