Tag: 0-100

Recyclable Palladium-Catalyzed Carbonylative Coupling of 2-Iodoanilines, Trimethyl Orthoformate, and Amines: A Practical Synthesis of Quinazolin-4(3H)-ones was written by Li, Jianying;Zhou, Zebiao;Xie, Gang;Cai, Mingzhong. And the article was included in Synthesis in 2022.Recommanded Product: 2-Methoxyethylamine The following contents are mentioned in the article:

An efficient heterogeneous palladium-catalyzed carbonylative annulation of 2-iodoanilines, tri-Me orthoformate, and amines has been developed. The reaction proceeds smoothly in toluene at 110°C using N,N-diisopropylethylamine (DiPEA) as base and 2 mol% of MCM-41-anchored bidentate phosphine palladium complex [MCM-41-2P-Pd(OAc)₂] as catalyst under 10 bar of carbon monoxide and provides a general and practical method for the construction of a wide variety of quinazolin-4(3H)-ones in good to excellent yields from com. easily available starting materials. This heterogenized palladium catalyst can be easily recovered via a simple centrifugation process and reused more than nine times with almost consistent catalytic efficiency. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Recommanded Product: 2-Methoxyethylamine).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Recommanded Product: 2-Methoxyethylamine

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro was written by Mambwe, Dickson;Kumar, Malkeet;Ferger, Richard;Taylor, Dale;Njoroge, Mathew;Coertzen, Dina;Reader, Janette;van der Watt, Mariette;Birkholtz, Lyn-Marie;Chibale, Kelly. And the article was included in ACS Medicinal Chemistry Letters in 2021.Recommanded Product: 109-85-3 The following contents are mentioned in the article:

In the context of drug repositioning and expanding the existing structure-activity relationship around astemizole (AST), a new series of analogs were designed, synthesized, and evaluated for their antiplasmodium activity. Among 46 analogs tested, compounds 21, 30, and 33 displayed high activities against asexual blood stage parasites (PfNF54 IC₅₀ = 0.025-0.043μM), whereas amide compound 46 addnl. showed activity against late-stage gametocytes (stage IV/V; PfLG IC₅₀ = 0.6 ± 0.1μM) and 860-fold higher selectivity over hERG (46, SI = 43) compared to AST. Several analogs displaying high solubility (Sol > 100μM) and low cytotoxicity in the Chinese hamster ovary (SI > 148) cell line have also been identified. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Recommanded Product: 109-85-3).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Recommanded Product: 109-85-3

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers was written by Irie, Takayuki;Asami, Tokiko;Sawa, Ayako;Uno, Yuko;Taniyama, Chika;Funakoshi, Yoko;Masai, Hisao;Sawa, Masaaki. And the article was included in Journal of Medicinal Chemistry in 2021.Formula: C3H9NO The following contents are mentioned in the article:

CDC7, a serine-threonine kinase, plays conserved and important roles in regulation of DNA replication and has been recognized as a potential anticancer target. We report here the optimization of a series of furanone analogs starting from compound 1 with a focus on ADME properties suitable for clin. development. By replacing the 2-chlorobenzene moiety in 1 with various aliphatic groups, we identified compound 24 as a potent CDC7 inhibitor with excellent kinase selectivity and favorable oral bioavailability in multiple species. Oral administration of 24 demonstrated robust in vivo antitumor efficacy in a colorectal cancer xenograft model. Compound 24 (AS-0141) is currently in phase I clin. trials for the treatment of solid cancers. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Structure-Based Design of Highly Potent Toll-like Receptor 7/8 Dual Agonists for Cancer Immunotherapy was written by Wang, Zhisong;Gao, Yan;He, Lei;Sun, Shuhao;Xia, Tingting;Hu, Lu;Yao, Licheng;Wang, Liangliang;Li, Dan;Shi, Hui;Liao, Xuebin. And the article was included in Journal of Medicinal Chemistry in 2021.COA of Formula: C3H9NO The following contents are mentioned in the article:

Design and synthesis of a series of pyrido[3,2-d]pyrimidine-based toll-like receptor 7/8 dual agonists, e.g., I that exhibited potent and near-equivalent agonistic activities toward TLR7 and TLR8. In vitro, compounds significantly induced the secretion of IFN-α, IFN-γ, TNF-α, IL-1β, IL-12p40, and IP-10 in human peripheral blood mononuclear cell assays. In vivo, compounds significantly suppressed tumor growth in CT26 tumor-bearing mice by remodeling the tumor microenvironment. Addnl., compounds markedly improved the antitumor activity of PD-1/PD-L1 blockade. These results demonstrated that TLR7/8 agonists held great potential as single agents or in combination with PD-1/PD-L1 blockade for cancer immunotherapy. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis was written by Frankowski, Kevin J.;Patnaik, Samarjit;Wang, Chen;Southall, Noel;Dutta, Dipannita;De, Soumitta;Li, Dandan;Dextras, Christopher;Lin, Yi-Han;Bryant-Connah, Marthe;Davis, Danielle;Wang, Feijun;Wachsmuth, Leah M.;Shah, Pranav;Williams, Jordan;Kabir, Md;Zhu, Edward;Baljinnyam, Bolormaa;Wang, Amy;Xu, Xin;Norton, John;Ferrer, Marc;Titus, Steve;Simeonov, Anton;Zheng, Wei;Mathews Griner, Lesley A.;Jadhav, Ajit;Aube, Jeffrey;Henderson, Mark J.;Rudloff, Udo;Schoenen, Frank J.;Huang, Sui;Marugan, Juan J.. And the article was included in Journal of Medicinal Chemistry in 2022.Computed Properties of C3H9NO The following contents are mentioned in the article:

A high-throughput, high-content assay was developed to identify novel small mols. that selectively reduce PNC prevalence in cancer cells. The pyrrolopyrimidine series able to reduce PNC prevalence in PC3M cancer cells at submicromolar concentrations without affecting cell viability was identified and further optimized. Structure-activity relationship exploration of the structural elements necessary for activity resulted in the discovery of several potent compounds Anal. of in vitro drug-like properties led to the discovery of the bioavailable analog, metarrestin, which has shown potent antimetastatic activity with improved survival in rodent models and is currently being evaluated in a first-in-human phase 1 clin. trial. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Computed Properties of C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Esters contain a carbonyl center, which gives rise to 120° C–C–O and O–C–O angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C–O–C bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Computed Properties of C3H9NO

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

[4 + 1] Annulation of in-situ generated azoalkenes with amines: A powerful approach to access 1-substituted 1,2,3-triazoles was written by Wang, Hongwei;Ning, Yongquan;Sivaguru, Paramasivam;Zanoni, Giuseppe;Bi, Xihe. And the article was included in Chinese Chemical Letters in 2022.Quality Control of 2-Methoxyethylamine The following contents are mentioned in the article:

Here a base-mediated [4 + 1] annulation of azoalkenes generated in-situ from readily available difluoroacetaldehyde N-tosylhydrazones (DFHZ-Ts) with amines under relatively mild conditions was reported. This azide- and acetylene-free strategy provides facile access to diverse 1-substituted 1,2,3-triazole derivatives in high yield in a regiospecific manner. This transformation was great functional group tolerance and was suit a broad substrate scope. Furthermore, the application of this novel methodol. in the gram-scale synthesis of an antibiotic drug PH-027 and in the late-stage derivatization of several bioactive small mols. and clin. drugs demonstrated its generality, practicability and applicability. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Quality Control of 2-Methoxyethylamine).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Liquid esters of low volatility serve as softening agents for resins and plastics. Esters also include many industrially important polymers. Polymethyl methacrylate is a glass substitute sold under the names Lucite and Plexiglas; polyethylene terephthalate is used as a film (Mylar) and as textile fibres sold as Terylene, Fortrel, and Dacron.Quality Control of 2-Methoxyethylamine

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Cobalt-catalyzed chemoselective dehydrogenation through radical translocation under visible light was written by Yu, Wan-Lei;Ren, Zi-Gang;Ma, Ke-Xing;Yang, Hui-Qing;Yang, Jun-Jie;Zheng, Haixue;Wu, Wangsuo;Xu, Peng-Fei. And the article was included in Chemical Science in 2022.COA of Formula: C3H9NO The following contents are mentioned in the article:

In this report, a straightforward and robust cobaloxime-catalyzed photochem. dehydrogenation strategy via intramol. HAT was described for the first time. The reaction proceeded through an intramol. radical translocation followed by the cobalt assisted dehydrogenation without needing any other external photosensitizers, noble-metals or oxidants. With this approach, a series of valuable unsaturated compounds such as α,β-unsaturated amides, enamides and allylic and homoallylic sulfonamides were obtained in moderate to excellent yields with good chemo- and regioselectivities, and the synthetic versatility was demonstrated by a range of transformations. And mechanistic studies of the method were discussed. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Dehydrocoupling of boranes with amines using a scandium catalyst was written by Wang, Yang;Xu, Pengfei;Xu, Xin. And the article was included in Chinese Chemical Letters in 2021.SDS of cas: 109-85-3 The following contents are mentioned in the article:

The scandocene alkyl complex (C₅Me₅)₂ScCH₂SiMe₃ was found to be an efficient catalyst for the dehydrocoupling of the non-cyclic boranes, dicyclohexylborane and thexylborane, with amines under mild conditions. The reactions afforded the corresponding aminoboranes in high yields with good functional group tolerance. The stoichiometric reaction of scandium alkyl with amine led to the isolation of a scandium amide complex, which was shown to be an active species during the catalysis. Although a borane-coordinated scandium hydride was also obtained from the stoichiometric experiment, it was not involved in the catalytic cycle. In addition, kinetic studies provided insight into this intermol. dehydrogenation reaction. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3SDS of cas: 109-85-3).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.SDS of cas: 109-85-3

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Electroselective and Controlled Reduction of Cyclic Imides to Hydroxylactams and Lactams was written by Bai, Ya;Shi, Lingling;Zheng, Lianyou;Ning, Shulin;Che, Xin;Zhang, Zhuoqi;Xiang, Jinbao. And the article was included in Organic Letters in 2021.HPLC of Formula: 109-85-3 The following contents are mentioned in the article:

An efficient and practical electrochem. method for selective reduction of cyclic imides has been developed using a simple undivided cell with carbon electrodes at room temperature The reaction provides a useful strategy for the rapid synthesis of hydroxylactams and lactams in a controllable manner, which is tuned by elec. current and reaction time, and exhibits broad substrate scope and high functional group tolerance even to reduction-sensitive moieties. Initial mechanistic studies suggest that the approach heavily relies on the utilization of amines (e.g., i-Pr₂NH), which are able to generate α-aminoalkyl radicals. This protocol provides an efficient route for the cleavage of C-O bonds under mild conditions with high chemoselectivity. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3HPLC of Formula: 109-85-3).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Esters contain a carbonyl center, which gives rise to 120° C–C–O and O–C–O angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C–O–C bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. HPLC of Formula: 109-85-3

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Discovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na⁺/H⁺ Exchanger Isoform 3 was written by Jacobs, Jeffrey W.;Leadbetter, Michael R.;Bell, Noah;Koo-McCoy, Samantha;Carreras, Christopher W.;He, Limin;Kohler, Jill;Kozuka, Kenji;Labonte, Eric D.;Navre, Marc;Spencer, Andrew G.;Charmot, Dominique. And the article was included in ACS Medicinal Chemistry Letters in 2022.COA of Formula: C3H9NO The following contents are mentioned in the article:

We present herein the design, synthesis, and optimization of gut-restricted inhibitors of Na⁺/H⁺ exchanger isoform 3 (NHE3). NHE3 is predominantly expressed in the kidney and gastrointestinal tract where it acts as the major absorptive sodium transporter. We desired minimally systemic agents that would block sodium absorption in the gastrointestinal tract but avoid exposure in the kidney. Starting with a relatively low-potency highly bioavailable hit compound (1), potent and minimally absorbed NHE3 inhibitors were designed, culminating with the discovery of tenapanor (28). Tenapanor has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of irritable bowel syndrome with constipation in adults. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3COA of Formula: C3H9NO).

2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.COA of Formula: C3H9NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem