Tag: 100-200

《Synthesis and cytotoxicity of thieno[2,3-b]pyridine derivatives toward sensitive and multidrug-resistant leukemia cells》 was published in Acta Chimica Slovenica in 2021. These research results belong to Al-Trawneh, Salah A.; Tarawneh, Amer H.; Gadetskaya, Anastassiya V.; Seo, Ean-Jeong; Al-Ta’ani, Mohammad R.; Al-Taweel, Samir A.; El-Abadelah, Mustafa M.. Formula: C7H13NO2 The article mentions the following:

A new series of substituted Et 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates I (R = H, CHO; X = H, 4-Me, 4-Cl; Y = O, S) were prepared by utilizing Et 2-chloro-7-cyclopropyl-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylate (1) and replacing of the 2-chlorine with anions obtained from phenol, salicylaldehyde derivatives like salicylaldehyde, 5-methylsalicylaldehyde and 5-chlorosalicylaldehyde or thiophenol, leading to the resp. Et 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates I. The new compounds I were evaluated for their in vitro cytotoxicity towards sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells. The screening revealed that compounds I (R = X = H, Y = O; R = CHO, X = H, Y = O; R = X = H, Y = S) inhibited the growth of both cell lines. Compound I (R = CHO, X = H, Y = O), with a phenol moiety, exhibited the highest growth inhibitory activity against CEM/ADR5000 and CCRF-CEM cells with IC50 values 4.486 ± 0.286 and 2.580 ± 0.550μM, resp. Collectively, the presented results demonstrate that the synthesized thieno[2,3-b]pyridines I warrant further exploration for potential use as anti-cancer agents. After reading the article, we found that the author used Ethyl 3-(dimethylamino)acrylate(cas: 924-99-2Formula: C7H13NO2)

Ethyl 3-(dimethylamino)acrylate(cas: 924-99-2) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Formula: C7H13NO2

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Ester – an overview | ScienceDirect Topics

《Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5-a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction》 was written by Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Yang, Linlin; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, MAA; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Wang, Shaomeng; Liu, Hong-Min. Application of 4949-44-4This research focused ontriazolo pyrimidine derivative preparation DCN1 UBC12 protein interaction cancer. The article conveys some information:

The cullin-RING ubiquitin ligases (CRLs) are responsible for about 20% of cellular protein degradation and regulate diverse cellular processes, and the dysfunction of CRLs is implicated in human diseases. Targeting the CRLs has become an emerging strategy for the treatment of human diseases. Herein, we describe the discovery of a hit compound from our inhouse library and further structure-based optimizations, which have enabled the identification of new triazolo[1,5-a]pyrimidine-based inhibitors targeting the DCN1-UBC12 interaction. Compound WS-383 blocks the DCN1-UBC12 interaction (IC50 = 11 nM) reversibly and shows selectivity over selected kinases. WS-383 exhibits cellular target engagement to DCN1 in MGC-803 cells. WS-383 inhibits Cul3/1 neddylation selectively over other cullins and also induces accumulation of p21, p27, and NRF2. Collectively, targeting the DCN1-UBC12 interaction would be a viable strategy for selective neddylation inhibition of Cul3/1 and may be of therapeutic potential for disease treatment in which Cul3/1 is dysregulated. After reading the article, we found that the author used Ethyl 3-oxopentanoate(cas: 4949-44-4Application of 4949-44-4)

Ethyl 3-oxopentanoate(cas: 4949-44-4) belongs to ketone compounds. They are most widely used as solvents, especially in industries manufacturing explosives, lacquers, paints, and textiles. Ketones are also used in tanning, as preservatives, and in hydraulic fluids.Application of 4949-44-4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Product Details of 609-08-5In 2019 ,《Substitution of the Dimethylamino Group in Gramines and One-Pot Cyclization to Tetrahydro-β-carbolines Using a Triazine-Based Activating Agent》 was published in Journal of Organic Chemistry. The article was written by Fujita, Hikaru; Nishikawa, Riho; Sasamoto, Ozora; Kitamura, Masanori; Kunishima, Munetaka. The article contains the following contents:

A new method for the substitution of 3-[(dimethylamino)methyl]indoles (gramines) with malonate-based nucleophiles was developed using 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) as the activating agent for the dimethylamino group. The reaction was completed in 1.5-6 h at room temperature in the presence of a tert-amine base and lithium salt. CDMT afforded superior results to Me iodide, a common activating agent for the dimethylamino group in Mannich bases, particularly in the reactions of 1-substituted gramines. The reactivity of the possible intermediates, bis(indol-3-ylmethyl)dimethylammonium salts, was examined to obtain mechanistic insights on the reaction. This substitution method with CDMT enabled the sequential transformation of gramines: substitution with (N-alkylidene)aminomalonates followed by the Pictet-Spengler reaction under acidic conditions afforded 1,2,3,4-tetrahydro-β-carboline derivatives in one pot. In the experiment, the researchers used Diethyl 2-methylmalonate(cas: 609-08-5Product Details of 609-08-5)

Diethyl 2-methylmalonate(cas: 609-08-5) belongs to aliphatic hydrocarbons. Aliphatic hydrocarbons belong to the most abundant fraction in crude oil. Aliphatics molecules are linear or branched open-chain structures such as n-alkanes, isoalkanes, cycloalkanes (naphthenes), terpenes and steranes.Product Details of 609-08-5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Synthetic Route of C8H14O4In 2019 ,《Ligand-Free, Quinoline N-Assisted Copper-Catalyzed Nitrene Transfer Reaction To Synthesize 8-Quinolylsulfimides》 appeared in Journal of Organic Chemistry. The author of the article were Xiao, Xinsheng; Huang, Sanping; Tang, Shanshan; Jia, Guokai; Ou, Guangchuan; Li, Yangyan. The article conveys some information:

In the presence of CuCN, 8-quinolinyl thioethers underwent regioselective imination via nitrene transfer reactions with sulfonyl azides to yield 8-quinolinyl sulfimides such as I (R = 4-MeC6H4, Ph, 4-ClC6H4, 4-BrC6H4, 4-F3CC6H4, 4-MeOC6H4, 4-MeCONHC6H4, 2-MeC6H4, 3-MeC6H4, 2,3,5,6-Me4C6H, 1-naphthyl, 2-thienyl, PhCH2, Me). I (R = 4-MeC6H4) was an effective ligand for allylic alkylation reactions of (E)-PhCH(OAc)CH:CHPh with 1,3-dicarbonyl compounds in the presence of PdCl2, N,O-bis(trimethylsilyl)acetamide, and KOAc. In the part of experimental materials, we found many familiar compounds, such as Diethyl 2-methylmalonate(cas: 609-08-5Synthetic Route of C8H14O4)

Diethyl 2-methylmalonate(cas: 609-08-5) belongs to aliphatic hydrocarbons. Aliphatic hydrocarbons belong to the most abundant fraction in crude oil. Aliphatics molecules are linear or branched open-chain structures such as n-alkanes, isoalkanes, cycloalkanes (naphthenes), terpenes and steranes.Synthetic Route of C8H14O4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

HPLC of Formula: 4755-77-5In 2021 ,《Quinazoline-containing hydrazydes of dicarboxylic acids and products of their structural modification: a novel class of anti-inflammatory agents》 appeared in Acta Chimica Slovenica. The author of the article were Krasovska, Nataliia; Stavytskyi, Viktor; Nosulenko, Inna; Karpenko, Oleksandr; Voskoboinik, Oleksii; Kovalenko, Serhii. The article conveys some information:

The synthesis of hydrazides formed by quinazolin-4(3H)-ylidenehydrazine and dicarboxylic acids, as well as their further modification are described in the present manuscript. It was shown that above-mentioned hydrazides may be obtained via acylation of initial quinazolin-4(3H)-ylidenehydrazine by corresponding acylhalides, cyclic anhydrides and imidazolides of dicarboxylic acids monoesters. Obtained hydrazides were converted into [1,2,4]triazolo[1,5-c]quinazolines that were used as initial compounds for chem. modification aimed to the introduction of amide fragment to the mol. The IR, 1H NMR and chromato-mass spectral data of obtained compounds were studied and discussed. Obtained substances were studied for anti-inflammatory activity using carrageenan-induced paw inflammation model. Amides of ([1,2,4]triazolo[1,5-c]quinazoline-2-yl)alkyl carboxylic acids were detected as promising class of anti-inflammatory agents for further purposeful synthesis and profound study of anti-inflammatory activity. In the experimental materials used by the author, we found Ethyl oxalyl monochloride(cas: 4755-77-5HPLC of Formula: 4755-77-5)

Ethyl oxalyl monochloride(cas: 4755-77-5) belongs to acyl chlorides. Lacking the ability to form hydrogen bonds, acyl chlorides have lower boiling and melting points than similar carboxylic acids. For example, acetic acid boils at 118 °C, whereas acetyl chloride boils at 51 °C. Like most carbonyl compounds, infrared spectroscopy reveals a band near 1750 cm−1.HPLC of Formula: 4755-77-5

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Recommanded Product: tert-Butyl carbamateIn 2021 ,《Copper(I)-catalyzed regioselective Ullmann-type coupling of primary carbamates and 5-substituted-1,2,3-triiodobenzenes: facile synthesis of 2,3-diiodinated N-aryl carbamates》 appeared in New Journal of Chemistry. The author of the article were Al-Zoubi, Raed M.; Al-Jammal, Walid K.; Al-Zoubi, Mazhar S.; McDonald, Robert; Zarour, Ahmad; Yassin, Aksam; Al-Ansari, Abdulla. The article conveys some information:

An efficient and unprecedented synthesis of 2,3-dihalo-N-phenylcarbamates through highly regioselective Ullmann-type C-N arylation reactions of 5-substituted-1,2,3-trihalobenzenes and primary carbamates was described. Remarkably, the amination reactions proceeded exclusively at the terminal positions the less sterically hindered, and the most regioactive positions. The highest yields were isolated from a combination between electron poor 1,2,3-triiodobenzenes and Et carbamates. The optimized conditions were found to be suitable for many functional groups. The first and unprecedented method to make 2,3-dihalo-N-phenylcarbamates that is efficient, general in scope, highly regioselective and gave truly remarkable precursors for other transformations.tert-Butyl carbamate(cas: 4248-19-5Recommanded Product: tert-Butyl carbamate) was used in this study.

tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Recommanded Product: tert-Butyl carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Category: esters-buliding-blocksIn 2022 ,《Hydrogenation of Esters by Manganese Catalysts》 appeared in Advanced Synthesis & Catalysis. The author of the article were Li, Xiao-Gen; Li, Fu; Xu, Yue; Xiao, Li-Jun; Xie, Jian-Hua; Zhou, Qi-Lin. The article conveys some information:

The hydrogenation of esters catalyzed by a manganese complex of phosphine-aminopyridine ligand was developed. Using this protocol, a variety of (hetero)aromatic and aliphatic carboxylates including biomass-derived esters and lactones were hydrogenated to primary alcs. R1CH2OH [R1 = Me, Ph, 2-furyl, etc.] with 63-98% yields. The manganese catalyst was found to be active for the hydrogenation of Me benzoate, providing benzyl alc. with turnover numbers (TON) as high as 45,000. Investigation of catalyst intermediates indicated that the amido manganese complex was the active catalyst species for the reaction. The experimental part of the paper was very detailed, including the reaction process of Methyl 4-fluorobenzoate(cas: 403-33-8Category: esters-buliding-blocks)

Methyl 4-fluorobenzoate(cas: 403-33-8) can be used in the synthesis of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH2-substituted benzyl moiety.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2022,Mekrattanachai, Pagasukon; Zhu, Lei; Setthaya, Naruemon; Chindawong, Chakkresit; Song, Wei Guo published an article in Catalysis Letters. The title of the article was 《The Highly Effective Cobalt Based Metal-Organic Frameworks Catalyst for One Pot Oxidative Esterification Under Mild Conditions》.Application In Synthesis of Methyl 4-fluorobenzoate The author mentioned the following in the article:

The cobalt-based metal organic frameworks (Co-MOFs) catalystwas prepared with using terephthalic acid and 4,4′-bipyridine as organic linkers by facile solvothermal method for one-pot oxidative esterification. The prepared catalyst was pyrolyzed at different temperature and then applied for oxidation of aldehyde using mol. oxygen as benign oxidant under mild conditions. The Co-MOFs pyrolyzed at 800 C (denoted as Co-MOFs-800) catalyst exhibited excellent catalytic activity, selectivity and recyclability toward the oxidative esterification of benzaldehydes. Furthermore, it was reused up to 5 runs without significant loss of activity. The experimental process involved the reaction of Methyl 4-fluorobenzoate(cas: 403-33-8Application In Synthesis of Methyl 4-fluorobenzoate)

Methyl 4-fluorobenzoate(cas: 403-33-8) is an organic fluorinated building block used for the synthesis of various pharmaceutical compounds. It can be used for the preparation of Blonanserin.Application In Synthesis of Methyl 4-fluorobenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Ni, Hangcheng; Li, Chaoming; Shi, Xingzi; Hu, Xianyue; Mao, Hui published an article in 2022. The article was titled 《Visible-Light-Promoted Fe(III)-Catalyzed N-H Alkylation of Amides and N-Heterocycles》, and you may find the article in Journal of Organic Chemistry.Application of 4248-19-5 The information in the text is summarized as follows:

A wide variety of amides RNH2 (R = benzoyl, 2-phenylacetyl, N-benzoylcarbamoyl, etc.) and nitrogen-containing heterocycles e.g., 1,3-dimethyl-3,9-dihydro-1H-purine-2,6-dione was tolerated in this protocol to give N-alkylated products I (R1 = H, Me; X = O, S) and e.g., II resp. The applicability of this protocol was further demonstrated by late-stage alkylation of N-H-containing pharmaceuticals. Moreover, N-H-alkylated α-amino tetrahydrofurans could be transformed into versatile ring-opened amino alcs. RNH(CH2)4OH under reducing conditions. A mechanistic study revealed that hydrogen atom transfer by a tert-butoxyl radical and a chlorine radical was responsible for the activation of C(sp3)-H precursors. The experimental process involved the reaction of tert-Butyl carbamate(cas: 4248-19-5Application of 4248-19-5)

tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Application of 4248-19-5

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Adamek, Jakub; Zielezny, Paulina; Erfurt, Karol published an article in 2021. The article was titled 《Synthesis of N-Protected 1-Aminoalkylphosphonium Salts from Amides, Carbamates, Lactams, or Imides》, and you may find the article in Journal of Organic Chemistry.Electric Literature of C5H11NO2 The information in the text is summarized as follows:

This report describes the development and optimization of the one-pot method for the synthesis of N-protected 1-aminoalkylphosphonium salts [R1CONR2CHR3P+Ar3]X based on the three-component coupling of aldehydes R3CHO and either amides, carbamates, lactams, imides, or ureas R1CONHR2 in the presence of triarylphosphonium salts [Ar3PH]X. The proposed strategy is very efficient and easy to carry out even on a larger scale (20 g) in any typical laboratory Most reactions occur at temperatures between 50 and 100° in a short time (1-2 h) without requiring any catalyst, and simple workup procedures afford good to excellent yields. The exceptions are condensations with imides, which require much higher temperatures (150-170°) and longer reaction times (even 30 h). The possibility of carrying out the synthesis under solvent-free conditions (neat reactions) is also demonstrated. Finally, we prove the developed one-pot methodol. can be successfully applied for the synthesis of structurally diverse N-protected 1-aminoalkylphosphonium salts. Mechanistic studies showed the intermediate products of described couplings are 1-hydroxyalkylphosphonium salts, not N-hydroxyalkylamides, -imides, etc., as initially expected. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl carbamate(cas: 4248-19-5Electric Literature of C5H11NO2)

tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Electric Literature of C5H11NO2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics