Tag: 100-200

《Indole: A Promising Scavenging Agent for Methylglyoxal and Related Carbonyls in Tryptophan Containing Maillard Model Systems》 was written by Ghassem Zadeh, Raheleh; Yaylayan, Varoujan. HPLC of Formula: 120-72-9This research focused ontryptophan Maillard model indole methylglyoxal carbonyl scavenging; carbonyl scavengers; formaldehyde; indole; methylglyoxal; phenylacetaldehyde and PhIP; tryptophan. The article conveys some information:

In situ generation of efficient carbonyl trapping agents from amino acids during food processing can be considered a useful approach to control the accumulation of harmful Maillard reaction products in food. Tryptophan is one such amino acid that can be used to generate carbonyl trapping agents. Indole, the main thermal degradation product of tryptophan, is known to react with simple aldehydes through electrophilic aromatic substitution type reactions mainly at carbon positions 2 and 3 in addition to the ring nitrogen. The ability of indole to scavenge three moles of reactive aldehydes per mol of indole such as formaldehyde, methylglyoxal, and phenylacetaldehyde was investigated using model systems containing tryptophan or indole. The model systems were either (a) heated in an aqueous solution in stainless steel reactors at specified time and temperatures and analyzed by qTOF-MS/MS or (b) directly pyrolyzed and analyzed by GC/MS using isotope labeling technique. Unlike the other aldehydes, the initial alc. formed with phenylacetaldehyde was able to dehydrate and form an stable conjugated system with the indole. In general, indole was able to capture three moles of paraformaldehyde, three moles of methylglyoxal and three moles of phenylacetaldehyde and suppress the formation of 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine (PhIP) generated in a model system. After reading the article, we found that the author used 1H-Indole(cas: 120-72-9HPLC of Formula: 120-72-9)

1H-Indole(cas: 120-72-9) belongs to indole. 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. 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.HPLC of Formula: 120-72-9

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

The author of 《Palladium-catalyzed regioselective C-H alkynylation of indoles with haloalkynes: access to functionalized 7-alkynylindoles》 were Fang, Songjia; Jiang, Guangbin; Li, Meng; Liu, Zhenying; Jiang, Huanfeng; Wu, Wanqing. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2019. Safety of 5-Fluoro-1H-indole The author mentioned the following in the article:

A Pd-catalyzed uniquely regioselective C-H alkynylation of indoles was described. In this protocol, simple and readily available haloalkynes are employed as efficient alkynylating reagents, affording functionalized 7-alkynylindoles in moderate to good yields. Also, further transformations of 7-alkynylated products were performed, which demonstrated the potential application of this method in organic synthesis. The results came from multiple reactions, including the reaction of 5-Fluoro-1H-indole(cas: 399-52-0Safety of 5-Fluoro-1H-indole)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Safety of 5-Fluoro-1H-indole

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

Liu, Jiang;Wang, Luyao;Guo, Na;Teng, Yu-Ou;Yu, Peng published 《Design, synthesis and biological evaluation of the novel isoindolinone derivatives》 in 2014. The article was appeared in 《Journal of Chemical and Pharmaceutical Research》. They have made some progress in their research.SDS of cas: 132680-54-7 The article mentions the following:

A series of novel isoindolinone derivatives I [R = morpholino, pyrrolidino, N-Boc-piperazino, piperazino] were designed, synthesized and screened for their antitumor activity against HT-29, K562 and HepG2 cell lines. Among the tested compounds, isoindolinone derivative I [R = N-Boc-piperazino] exhibited good antitumor activity against HepG2 cancer cell line with IC₅₀ of 5.89 μM. And 6-Methoxyisoindolin-1-one (cas: 132680-54-7) was used in the research process.

The crystal structure of 6-Methoxyisoindolin-1-one(cas:132680-54-7 SDS of cas: 132680-54-7) has been determined using x-ray crystallography and cell studies. It was found that 6-Methoxyisoindolin-1-one inhibits the interactions of chk1 with substructures of DNA, such as the major groove and minor groove.

Reference:
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

Smith, Keith;El-Hiti, Gamal A.;Hegazy, Amany S.;Kariuki, Benson published 《A simple and convenient one-pot synthesis of substituted isoindolin-1-ones via lithiation, substitution and cyclization of N’-benzyl-N,N-dimethylureas》. The research results were published in《Beilstein Journal of Organic Chemistry》 in 2011.Category: indole-building-block The article conveys some information:

Lithiation of N’-benzyl-N,N-dimethylurea and its substituted derivatives with (tert-butyl)lithium (3.3 equiv) in anhydrous THF at 0° followed by a reaction with various electrophiles afforded a range of 3-substituted isoindolinone derivatives in high yields.6-Methoxyisoindolin-1-one (cas: 132680-54-7) were involved in the experimental procedure.

6-Methoxyisoindolin-1-one(cas:132680-54-7 Category: indole-building-block) also interacts with inhibitors of other topoisomerases such as camptothecin and etoposide. It has been shown that combining these two drugs can inhibit cancer cells more effectively than either drug alone.

Reference:
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

Ma, Rui-Jun;Xu, Wen-Ke;Sun, Jian-Ting;Chen, Ling;Si, Chang-Mei;Wei, Bang-Guo published 《Synthesis of dihydro-[1,3]oxazino[4,3-a] isoindole and tetrahydroisoquinoline through Cu(OTf)₂-catalyzed reactions of N-acyliminium ions with ynamides》 in 2021. The article was appeared in 《Tetrahedron Letters》. They have made some progress in their research.Related Products of 132680-54-7 The article mentions the following:

An efficient approach to access functionalized dihydro-[1,3]oxazino[4,3-a] isoindole and tetrahydroisoquinoline skeletons has been developed through the addition-cyclization process of ynamides with N-acyliminium ions generated from N,O-acetals. The reactions were conducted under the catalysis of Cu(OTf)₂, and a number of functionalized dihydro-[1,3]oxazino[4,3-a] isoindoles and tetrahydroisoquinolines were generated in 48-98% yields. When chiral ynamides were used, optically pure tetrahydroisoquinolines could be obtained with good to excellent yields and diastereoselectivities. And 6-Methoxyisoindolin-1-one (cas: 132680-54-7) was used in the research process.

6-Methoxyisoindolin-1-one(cas:132680-54-7 Related Products of 132680-54-7) also interacts with inhibitors of other topoisomerases such as camptothecin and etoposide. It has been shown that combining these two drugs can inhibit cancer cells more effectively than either drug alone.

Reference:
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

Girijavallabhan, Vinay M.;Chen, Lei;Dai, Chaoyang;Feltz, Robert J.;Firmansjah, Luke;Li, Dansu;Kim, Seong Heon;Kozlowski, Joseph A.;Lavey, Brian J.;Kosinski, Aneta;Piwinski, John J.;Popovici-Muller, Janeta;Rizvi, Razia;Rosner, Kristin E.;Shankar, Banderpalle B.;Shih, Neng-Yang;Siddiqui, M. Arshad;Tong, Ling;Wong, Michael K. C.;Yang, De-yi;Yang, Liping;Yu, Wensheng;Zhou, Guowei;Guo, Zhuyan;Orth, Peter;Madison, Vincent;Bian, Hong;Lundell, Daniel;Niu, Xiaoda;Shah, Himanshu;Sun, Jing;Umland, Shelby published 《Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases》. The research results were published in《Bioorganic & Medicinal Chemistry Letters》 in 2010.Reference of 6-Methoxyisoindolin-1-one The article conveys some information:

Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K _i) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors such as 37 (I) with good DMPK profiles. The experimental procedure involved many compounds, such as 6-Methoxyisoindolin-1-one (cas: 132680-54-7) .

6-Methoxyisoindolin-1-one(cas:132680-54-7 Reference of 6-Methoxyisoindolin-1-one) also interacts with inhibitors of other topoisomerases such as camptothecin and etoposide. It has been shown that combining these two drugs can inhibit cancer cells more effectively than either drug alone.

Reference:
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

Ma, Rui-Jun;Sun, Jian-Ting;Liu, Chang-Hong;Chen, Ling;Si, Chang-Mei;Wei, Bang-Guo published 《Synthesis of 1-benzylisoindoline and 1-benzyl-tetrahydroisoquinoline through nucleophilic addition of organozinc reagents to N,O-acetals》. The research results were published in《Organic & Biomolecular Chemistry》 in 2020.Name: 6-Methoxyisoindolin-1-one The article conveys some information:

A new approach to access 1-benzylisoindolines I [n = 1, 2; R¹ = Bn, 4-FC₆H₄CH₂, 4-t-BuC₆H₄CH₂, etc.; R² = H, 5-Br, 6-Cl, etc.] and 1-benzyl-tetrahydroisoquinolines I [R² = H, 6,7-di-OMe] was developed through nucleophilic addition of organozinc reagents to N,O-acetals. A number of substituted organozinc reagents were amenable for this transformation, and the desired products were obtained with excellent yields. Moreover, Sc(OTf)₃ proved to be an effective catalyst for the formation of 1-benzylisoindolines I and 1-benzyl-tetrahydroisoquinolines II using such nucleophilic addition And 6-Methoxyisoindolin-1-one (cas: 132680-54-7) was used in the research process.

6-Methoxyisoindolin-1-one(cas:132680-54-7 Name: 6-Methoxyisoindolin-1-one) is a class III topoisomerase inhibitor that binds to the chk1 protein, which is an enzyme involved in DNA replication. 6-Methoxyisoindolin-1-one inhibits the interaction between the chk1 protein and DNA, preventing DNA replication.

Reference:
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

Lopez-Valdez, German;Olguin-Uribe, Simon;Miranda, Luis D. published 《Carbamoyl radicals from carbamoylxanthates: a facile entry into isoindolin-1-ones》 in 2007. The article was appeared in 《Tetrahedron Letters》. They have made some progress in their research.Formula: C9H9NO2 The article mentions the following:

It has been found that carbamoylxanthates (e.g., BnN(CMe₃)C(O)S₂COEt) derived from secondary t-Bu amines are stable compounds which function as efficient sources of carbamoyl radicals. The carbamoylxanthates derived from t-butylbenzylamines can be efficiently transformed into 2-t-butylisoindolin-1-ones (e.g. I) via an oxidative radical cyclization process. The carbamoylxanthates derived from N-t-butylamino olefins underwent the expected cyclization/xanthate-transfer process to afford the corresponding pyrrolidones and piperidones under thermally induced DLP fragmentation conditions and in the presence of catalytic Et₃B in air, at room temperature The experimental procedure involved many compounds, such as 6-Methoxyisoindolin-1-one (cas: 132680-54-7) .

6-Methoxyisoindolin-1-one(cas:132680-54-7 Formula: C9H9NO2) also interacts with inhibitors of other topoisomerases such as camptothecin and etoposide. It has been shown that combining these two drugs can inhibit cancer cells more effectively than either drug alone.

Reference:
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

Electric Literature of C9H9NO2In 2017, Ling, Fei;Ai, Chongren;Lv, Yaping;Zhong, Weihui published 《Traceless Directing Group Assisted Cobalt-Catalyzed C-H Carbonylation of Benzylamines》. 《Advanced Synthesis & Catalysis》published the findings. The article contains the following contents:

An expedient and convenient strategy was reported for regioselective synthesis of N-unprotected isoindolinones I [R¹ = H, 6-Me, 4-Br, etc.; R² = H, Et, Ph, etc.] via Co-catalyzed C(sp²)-H carbonylation of benzylamines II using picolinamide as traceless directing group through direct C-H/N-H bond activation using DEAD as environmentally benign carbonyl source. This carbonylation strategy was also compatible with various aryl/heteroaryl substituted amines that afforded corresponding N-unprotected isoindolinones, e.g., III, thieno[2,3-c]pyrrol-4-one and 3,4-dihydroisoquinolin-1(2H)-one. This protocol tolerated a variety of functional groups and provided a facile and efficient method for the formal synthesis of (+)-garenoxacin. The experimental procedure involved many compounds, such as 6-Methoxyisoindolin-1-one (cas: 132680-54-7) .

6-Methoxyisoindolin-1-one(cas:132680-54-7 Electric Literature of C9H9NO2) also interacts with inhibitors of other topoisomerases such as camptothecin and etoposide. It has been shown that combining these two drugs can inhibit cancer cells more effectively than either drug alone.

Reference:
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

Barnes, Keith D.;Chen, Ping;Chang, Yingyan;Lewis, Robert M.;Manley, Christopher M.;Mayhew, Nicholas J.;Steffke, Stephen H.;Wang, Guixing;Wang, Yi;Yang, Yuh-Lin A.;Lippert, John W. III published 《Lactam coupling as a versatile route to indoprofen analogs》 in 2011. The article was appeared in 《Synthetic Communications》. They have made some progress in their research.Reference of 6-Methoxyisoindolin-1-one The article mentions the following:

A convergent synthesis of indoprofen via a palladium-catalyzed Buchwald-Hartwig cross-coupling approach was reported. Using this methodol., indoprofen and a set of analogs of indoprofen were readily prepared6-Methoxyisoindolin-1-one (cas: 132680-54-7) were involved in the experimental procedure.

The crystal structure of 6-Methoxyisoindolin-1-one(cas:132680-54-7 Reference of 6-Methoxyisoindolin-1-one) has been determined using x-ray crystallography and cell studies. It was found that 6-Methoxyisoindolin-1-one inhibits the interactions of chk1 with substructures of DNA, such as the major groove and minor groove.

Reference:
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