Month: November 2022

Wang, Liang; Zhu, Kai-qiang; Wu, Wen-ting; Chen, Qun; He, Ming-yang published an article in 2015, the title of the article was n-Bu4NI-catalyzed direct amination of ethers with aryl tetrazoles and triazoles via cross-dehydrogenative coupling reaction.HPLC of Formula: 5301-96-2 And the article contains the following content:

An efficient, metal-free protocol for direct amination of ethers with aryl tetrazoles and triazoles has been developed using tetrabutylammonium iodide (TBAI) as a catalyst and tert-Bu hydroperoxide (t-BuOOH) as an oxidant. A series of ethers, aryl tetrazoles as well as triazoles are tolerated in this system, giving the corresponding products in moderate to good yields. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).HPLC of Formula: 5301-96-2

The Article related to amination ether aryltetrazole aryltriazole cross dehydrogenative coupling, metal free amination tetrabutylammonium iodide catalyst tertbutyl hydroperoxide oxidant, Heterocyclic Compounds (More Than One Hetero Atom): General and other aspects.HPLC of Formula: 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Ma, Jiliang; Peng, Xinwen; Zhong, Linxin; Sun, Runcang published an article in 2018, the title of the article was Sulfonation of carbonized xylan-type hemicellulose: a renewable and effective biomass-based biocatalyst for the synthesis of O- and N-heterocycles.HPLC of Formula: 5301-96-2 And the article contains the following content:

The application of biomass-based carbonaceous solid acids in catalysis is attracting increasing attention in the field of chem. In this study, a heterogeneous carbon-based solid acid biocatalyst (CXH-SO3H) with regular spherical structure was synthesized from xylan-type hemicellulose (XH) by a simple two-step method. The catalyst was successfully applied in the synthesis of O- and N-heterocycles with yields of 80-99% and 60-97%, resp. In view of environment and economy, CXH-SO3H shows the merits of environmental friendliness, easy operation, simple work-up, excellent yields, and the avoidance of use of organic solvents and expensive catalysts. Moreover, the as-synthesized solid acid catalyst could be used for several cycles without significant loss in its catalytic activity. The results of FT-IR, XRD, and SEM showed that no distinct differences in physico-chem. structures of CXH-SO3H were observed Thus, the eco-friendly CXH-SO3H catalyst is a promising candidate for green synthesis of O- and N-heterocycles from low-cost feed-stocks and has good prospect in partially substituting com. available solid and liquid acid catalysts and precious metal catalysts. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).HPLC of Formula: 5301-96-2

The Article related to sulfonation carbonized xylan hemicellulose renewable biocatalyst o n heterocycle, Cellulose, Lignin, Paper, and Other Wood Products: Cellulose and other aspects.HPLC of Formula: 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Luo, Guoli; Sun, Chenyang; Li, Yan; Li, Xiaoxiao; Zhao, Zhigang published an article in 2018, the title of the article was N2-selective alkylation of NH-1,2,3-triazoles with vinyl ethers via gold catalysis.Computed Properties of 5301-96-2 And the article contains the following content:

A new method was developed to synthesize N2-alkyl-substituted 1,2,3-triazoles via gold catalyzed alkylation of vinyl ethers with mono- and unsubstituted NH-1,2,3-triazoles and benzotriazole. A hydrogen bond between the oxygen atom of the vinyl ethers, activated via the gold catalyst, and the NH-1,2,3-triazoles was supposed to be generated, which selectively gave the N2-alkylation products. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Computed Properties of 5301-96-2

The Article related to alkyltriazole preparation, triazole vinyl ether gold catalyst regioselective alkylation, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Computed Properties of 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On May 31, 1980, Boev, V. I.; Kushnir, V. N.; Shevchuk, M. I.; Dombrovskii, A. V. published an article.Recommanded Product: 5301-96-2 The title of the article was Synthesis and properties of 1,2,3-triazoles containing a ferrocenyl nucleus. And the article contained the following:

The title compounds I (R1 = H, Me, MeO, Cl, Br, NO2, R2 = H; R1 = H, R2 = Me; Fc = ferrocenyl) were prepared in 57-77% yields by cyclizing Ph3P:CR2COR1 with FcSO2N3. Treating I with EtOH gave 96-99% II. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Recommanded Product: 5301-96-2

The Article related to ferrocenyl triazole, triazole ferrocenylsulfonyl, Organometallic and Organometalloidal Compounds: Iron Compounds and other aspects.Recommanded Product: 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On July 15, 2010, Oh, Sangtae; Shin, Woon-Seob; Ham, Jungyeob; Lee, Seokjoon published an article.HPLC of Formula: 5301-96-2 The title of the article was Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells. And the article contained the following:

A diastereomeric and regioisomeric library of 10-triazolylartemisinins with potent growth-inhibitory activities against various cancer cell lines was established. These compounds were synthesized by the reaction with dihydroartemisinin and various triazoles in CH2Cl2 using BF3.OEt2 catalyst. Most of the compounds exhibited a strong potency in the submicromolar range, and, in particular, 3 compounds, having a (pentylphenyl)triazole moiety, proved to be promising candidates for preclin. trials. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).HPLC of Formula: 5301-96-2

The Article related to triazole artemisinin preparation anticancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.HPLC of Formula: 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On February 20, 2011, Lee, Seokjoon published an article.Synthetic Route of 5301-96-2 The title of the article was Synthesis of 10β-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells. And the article contained the following:

A library of 10-triazolylartemisinins was established comprising compounds that strongly inhibit the growth of cancer cell lines, such as DLD-1, U-87, Hela, SiHa, A172, and Bi1. These compounds were synthesized by an acid-catalyzed reaction of dihydroartemisinin (I) with various triazoles in CH2Cl2 at room temperature In particular, when 3 equivalent of triazole were reacted with I, 10β-(4-substituted triazolyl)artemisinins were obtained, which means that the type of product obtained differs according to the quantity of triazole reactant employed in the synthesis. From the viewpoint of antiproliferative activity against the various cancer cells, compounds, which have a (pentylphenyl)triazole moiety, exhibited potent activity. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Synthetic Route of 5301-96-2

The Article related to triazolylartemisinin preparation anticancer, artemisinin triazole preparation anticancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.Synthetic Route of 5301-96-2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On March 18, 2021, Mitsiades, Constantine S.; Shirasaki, Ryosuke; Matthews, Geoffrey M.; Gandolfi, Sara; De Matos Simoes, Ricardo published a patent.Formula: C49H60ClN9O7S2 The title of the patent was Methods for treating cancer using serial administration of E3 ubiquitin ligase degraders. And the patent contained the following:

The present invention relates, in part, to methods for treating cancer using serial administration of E3 ubiquitin ligase degraders. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Formula: C49H60ClN9O7S2

The Article related to e3 ubiquitin ligase degrader cancer therapy, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C49H60ClN9O7S2

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On May 19, 2021, Liu, Jing; Chen, He; Liu, Yi; Shen, Yudao; Meng, Fanye; Kaniskan, H. Umit; Jin, Jian; Wei, Wenyi published an article.Synthetic Route of 1949837-12-0 The title of the article was Cancer Selective Target Degradation by Folate-Caged PROTACs. And the article contained the following:

PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin-proteasome system. However, potential toxicity of PROTACs in normal cells due to the off-tissue on-target degradation effect limits their clin. applications. Precise control of a PROTAC’s on-target degradation activity in a tissue-selective manner could minimize potential toxicity/side-effects. To this end, we developed a cancer cell selective delivery strategy for PROTACs by conjugating a folate group to a ligand of the VHL E3 ubiquitin ligase, to achieve targeted degradation of proteins of interest (POIs) in cancer cells vs. noncancerous normal cells. We show that our folate-PROTACs, including BRD PROTAC (folate-ARV-771), MEK PROTAC (folate-MS432), and ALK PROTAC (folate-MS99), are capable of degrading BRDs, MEKs, and ALK, resp., in a folate receptor-dependent manner in cancer cells. This design provides a generalizable platform for PROTACs to achieve selective degradation of POIs in cancer cells. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Synthetic Route of 1949837-12-0

The Article related to preparation folate caged protac cancer toxicity, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On February 28, 2018, Sun, B.; Fiskus, W.; Qian, Y.; Rajapakshe, K.; Raina, K.; Coleman, K. G.; Crew, A. P.; Shen, A.; Saenz, D. T.; Mill, C. P.; Nowak, A. J.; Jain, N.; Zhang, L.; Wang, M.; Khoury, J. D.; Coarfa, C.; Crews, C. M.; Bhalla, K. N. published an article.Synthetic Route of 1949837-12-0 The title of the article was Bet protein proteolysis targeting chimera (protac) exerts potent lethal activity against mantle cell lymphoma cells. And the article contained the following:

Bromodomain extraterminal protein (BETP) inhibitors transcriptionally repress oncoproteins and nuclear factor-κB (NF-κB) target genes that undermines the growth and survival of mantle cell lymphoma (MCL) cells. However, BET bromodomain inhibitor (BETi) treatment causes accumulation of BETPs, associated with reversible binding and incomplete inhibition of BRD4 that potentially compromises the activity of BETi in MCL cells. Unlike BETi, BET-PROTACs (proteolysis-targeting chimera) ARV-825 and ARV-771 (Arvinas, Inc.) recruit and utilize an E3-ubiquitin ligase to effectively degrade BETPs in MCL cells. BET-PROTACs induce more apoptosis than BETi of MCL cells, including those resistant to ibrutinib. BET-PROTAC treatment induced more perturbations in the mRNA and protein expressions than BETi, with depletion of c-Myc, CDK4, cyclin D1 and the NF-κB transcriptional targets Bcl-xL, XIAP and BTK, while inducing the levels of HEXIM1, NOXA and CDKN1A/p21. Treatment with ARV-771, which possesses superior pharmacol. properties compared with ARV-825, inhibited the in vivo growth and induced greater survival improvement than the BETi OTX015 of immune-depleted mice engrafted with MCL cells. Cotreatment of ARV-771 with ibrutinib or the BCL2 antagonist venetoclax or CDK4/6 inhibitor palbociclib synergistically induced apoptosis of MCL cells. These studies highlight promising and superior preclin. activity of BET-PROTAC than BETi, requiring further in vivo evaluation of BET-PROTAC as a therapy for ibrutinib-sensitive or -resistant MCL. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).Synthetic Route of 1949837-12-0

The Article related to mantle cell lymphoma antitumor bet protein proteolysis, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On February 13, 2020, Bernstein, Bradley E.; Doench, John G.; Najm, Fadi J. published a patent.SDS of cas: 1949837-12-0 The title of the patent was Methods of combinatorial drug screening and use of therapeutic targets thereof in cancer treatment. And the patent contained the following:

CRISPR-Cas9 has enabled a new generation of screening strategies to interrogate gene function. However, redundant genes and the complexity of functional gene networks can confound single gene knockout approaches. Furthermore, simple addition of two or more sgRNAs has shown only modest targeting efficacy in screening approaches. The present invention relates to combined orthogonal CRISPR-derived components to maximize gene targeting activity with minimal cross-talk and interference. The present invention also relates to efficient S. aureus Cas9 sgRNA design rules, which were paired with S. pyogenes Cas9 sgRNA design rules to achieve dual target gene inactivation in a high fraction of cells. Applicants developed a lentiviral vector and cloning strategy to generate high complexity pooled dual-knockout libraries and show that screening these libraries can identify combinatorial phenotypes, including synthetic lethal gene pairs across multiple cell types. The gene pairs can be targeted therapeutically and applicants disclose therapeutically effective combination therapies using agents such as AZD5153, CPI-203, OTX015, JQ1. The experimental process involved the reaction of (2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide(cas: 1949837-12-0).SDS of cas: 1949837-12-0

The Article related to antitumor screening therapeutic drug target cancer treatment, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 1949837-12-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics