Tag: 100-200

On October 22, 2019, Xiang, Hua; Teng, Yu; Zou, Yumei; Lin, Xin; Wang, Xuening; Shen, Hongtao; Cheng, Yu; Ha, Si; Tong, Chao; Wang, Han published a patent.Quality Control of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of benzopyrimidine compounds useful as Btk or PI3K kinase inhibitors for the treatment of cancer. And the patent contained the following:

The invention relates to benzopyrimidine compounds of formula I and II, method for their preparation and their use as Btk or PI3K kinase inhibitors for the treatment of cancer. Compounds of formula I and II, wherein ring A is (hetero)aryl; R2 is H, C1-3alkyl, C1-3alkoxy, halo, etc.l R3 is H and Me; X is C, O and N; R3 is R4CONH; R4 is C1-4alkyl, C2-4alkeny and C2-4alkynyl; A is (CH2)2-4, and their pharmaceutically acceptable salts, are claimed. Example compound III was prepared via a multistep procedure (procedure given). The above compounds can be used for preparing Btk or PI3K kinase inhibitors to treat or prevent diseases related to protein kinase activity, including tumors, such as leukemias and lymphomas. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Quality Control of N-(3-Aminophenyl)acrylamide

The Article related to benzopyrimidine preparation btk pi3k kinase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide

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

Jain, Preeti; Kumar, Anil published an article in 2018, the title of the article was Structural Elucidation of the Binary Mixtures of [EMIM][BF4] and [BMIM][BF4] in Ethyl-Substituted Solvents by Isothermal Titration Calorimeter.Category: amides-buliding-blocks And the article contains the following content:

In order to address the issue whether both ionic liquids and solvents influence the enthalpy of their solutions, highly accurate excess partial molar enthalpy, HILE values have been measured using Isothermal Titration Calorimeter (ITC). Therefore, thermodn. behavior has been observed in the mixtures containing ionic liquids It essentially depends on the mol. structure of the constituents of the mixture The hydrogen bonding between ionic liquids and ethyl-substituted solvents (2-ethoxyethanol, ethylene glycol, diethylamine, Et acetate and N,N- diethylacetamide) may lead to strong ion-solvent interactions. In the present study, an effort has been made to quantify various interactions between ionic liquid and solvent, based on the HILE values. Linear solvation free relation shows dependence of limiting excess partial molar enthalpies, HILE,∞ upon the solvent properties. Structural orientation of solvent mols. and ionic liquids also described by the HILE,∞ values. The ion-ion, ion-solvent interactions have also been investigated in terms of the enthalpic interaction parameters, HIL-ILE and relative apparent molar enthalpy, φL of ionic liquid-ethyl-substituted solvent systems. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Category: amides-buliding-blocks

The Article related to solvent ionic liquid binary mixture structural elucidation, Thermodynamics, Thermochemistry, and Thermal Properties: Thermochemical Properties and other aspects.Category: amides-buliding-blocks

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

On November 1, 2019, Zaitseva, Ksenia V.; Varfolomeev, Mikhail A.; Verevkin, Sergey P. published an article.HPLC of Formula: 685-91-6 The title of the article was Vapour pressures and enthalpies of vaporisation of N,N-di-alkyl-acetamides. And the article contained the following:

Molar enthalpies of vaporisation of N,N-di-alkyl-acetamides (alkyl = Me, Et, Bu, and n-hexyl) were obtained from the temperature dependence of the vapor pressure measured using the transpiration method. A large number of primary exptl. results on temperature dependencies of vapor pressures have been collected from the literature and have been treated uniformly in order to derive vaporisation enthalpies at the reference temperature 298.15 K. The evaluated data were checked for internal consistency successfully. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).HPLC of Formula: 685-91-6

The Article related to dialkyl acetamide vapor pressure enthalpy vaporization, Thermodynamics, Thermochemistry, and Thermal Properties: Thermochemical Properties and other aspects.HPLC of Formula: 685-91-6

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

Zhang, Feng-Hua; Wang, Chen; Xie, Jian-Hua; Zhou, Qi-Lin published an article in 2019, the title of the article was Synthesis of Tridentate Chiral Spiro Aminophosphine-Oxazoline Ligands and Application to Asymmetric Hydrogenation of α-Keto Amides.Category: amides-buliding-blocks And the article contains the following content:

A new type of tridentate chiral spiro aminophosphine-oxazoline ligands (SpiroOAP) were synthesized through four steps. The SpiroOAP ligands are highly efficient for the asym. hydrogenation of α-keto amides, providing a variety of synthetically useful α-hydroxy amides with excellent enantioselectivity (up to 98% ee) and turnover numbers (up to 10,000). The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Category: amides-buliding-blocks

The Article related to chiral spiro aminophosphine oxazoline ligand preparation, keto amide aminophosphine oxazoline iridium catalyst enantioselective hydrogenation, hydroxy amide preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Alcohols and Thiols and other aspects.Category: amides-buliding-blocks

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

On February 28, 2007, Galenko, A. V.; Lobanov, P. S.; Potekhin, A. A. published an article.Name: 2-Amino-6-methylnicotinamide The title of the article was Reactions of α-tosyl- and α-cyanoacetamidoximes with 1,3-dicarbonyl compounds. And the article contained the following:

Cyclocondensation of α-tosylacetamidoxime and α-cyanoacetamidoxime with 1,3-dicarbonyl compounds affords the corresponding pyrimidine N-oxides. The 2-(cyanomethyl)pyrimidine-3-oxides isolated readily undergo cyclization to isoxazolopyrimidinium salts via intramol. addition of N-oxide to the nitrile group under acidic conditions. The experimental process involved the reaction of 2-Amino-6-methylnicotinamide(cas: 100524-09-2).Name: 2-Amino-6-methylnicotinamide

The Article related to isoxazolopyrimidinium preparation ring opening, pyrimidine oxide cyano preparation intramol cycloaddition, acetamidoxime cyclocondensation dicarbonyl compound, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-Amino-6-methylnicotinamide

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

On June 16, 2017, Song, Zhendong; Huang, Shanshan; Yu, Haiqing; Jiang, Yu; Wang, Changyuan; Meng, Qiang; Shu, Xiaohong; Sun, Hunjun; Liu, Kexin; Li, Yanxia; Ma, Xiaodong published an article.Category: amides-buliding-blocks The title of the article was Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). And the article contained the following:

Potential new EGFRT790M inhibitors comprising of structurally modified diphenylpyrimidine derivatives bearing a morpholine functionality (Mor-DPPYs), e.g., I were synthesized and used to improve the activity and selectivity of gefitinib-resistant non-small cell lung cancer (NSCLC) treatment. This led to the identification of inhibitor I, which displayed high activity against EGFRT790M/L858R kinase (IC50 = 0.71 nM) and repressed H1975 cell replication harboring EGFRT790M mutations at a concentration of 0.037 μM. Inhibitor I demonstrated high selectivity (SI = 631.9) for T790M-containing EGFR mutants over wild type EGFR and suggested that it will cause few side effects. Moreover, this compound also shows promising antitumor efficacy in a murine EGFRT790M/L858R-driven H1975 xenograft model without affecting body weight This study provides new potential lead compounds for further development of anti-NSCLC drugs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to acrylamide diphenylaminopyrimidinyl morpholino preparation antitumor egfr kinase mol modeling, egfr t790m, inhibitors, nsclc, pyrimidine, resistance, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

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

On May 1, 2012, Takahashi, Daisuke; Honda, Yutaka; Izawa, Kunisuke published an article.Product Details of 27115-50-0 The title of the article was Syntheses of 5-amino-2-phenyl-4(3H)-pyrimidinone derivatives starting with glycine. And the article contained the following:

N-Cbz-5-amino-2-phenyl-4(3H)-pyrimidinone was prepared from the Na salt of Me (hydroxymethylene)glycinate and benzamidine.HCl in good yield. However, the reaction with N-substituted benzamidine did not proceed to give the desired pyrimidinone. In contrast, the reaction of 4-ethoxymethylene-2-phenyl-5(4H)-oxazolone, readily prepared from hippuric acid and N-substituted benzamidine, proceeded nicely to give 5-(benzoylamino)-6-oxo-2-phenyl-1(6H)-pyrimidineacetate in high yield. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Product Details of 27115-50-0

The Article related to glycine benzamidine cyclocondensation, hippuric acid benzamidine cyclocondensation, aminopyrimidinone preparation, pyrimidinone amino preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 27115-50-0

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

On August 1, 2021, Wang, Zhengjie; Liu, Limin; Dai, Honglin; Si, Xiaojie; Zhang, Luye; Li, Erdong; Yang, Zhang; Chao, Gao; Zheng, Jiaxin; Ke, Yu; Shan, Lihong; Zhang, Qiurong; Liu, Hongmin published an article.Related Products of 16230-24-3 The title of the article was Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway. And the article contained the following:

In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound I had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound I also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound I exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound I could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound I targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Mol. docking showed that compound I could bind into the active pocket of EGFR. Those work suggested that compound I would have remarkable implications for further design of anti-tumor agents. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Related Products of 16230-24-3

The Article related to quinazoline preparation antiproliferation antitumor mol docking apoptosis egfr, antiproliferation, cell cycle analysis, egfr, quinazoline, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 16230-24-3

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

On December 27, 2018, Cho, Seong Yun; Kim, Pil Ho; Lee, Jeong Ok; Kim, Hyeong Rae; Ha, Jae Du; Jung, Hui Jeong; Yoon, Chang Su; Park, Ji Hun; Hwang, Jong Yeon published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Fused pyrimidine derivative as Bruton’s tyrosine kinase inhibitor, and method for the preparation thereof. And the patent contained the following:

Disclosed are compound I [n = 0 or 1; A = single bond, -NH- or -O-; D1 = CR4 or N; R4 = H or alkyl; D2 = CH or N; D3 = N or NH; a dotted line accompanied by a solid line represents a single bond or a double bond; R1 = (un)substituted aryl; R2, R3 = independently H, (un)substituted aryl, (un)substituted cycloalkyl, etc.; or its optical isomer or pharmaceutically acceptable salt] and pharmaceutical compositions For example, compound II was prepared from malononitrile via conversion to 4,6-dichloro-3-methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine followed by treatment with K2CO3/N-(1s,4s)-(4-aminocyclohexyl)acrylamide and Pd2(dba)3-catalyzed reaction with 4-morpholinoaniline. The invention compound showed high inhibitory activity for Bruton’s tyrosine kinase (BTK), e.g., IC50 value of II was 0.001 μM. Compound I is claimed useful for the treatment of cancer or autoimmune disease. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide

The Article related to fused pyrimidine preparation bruton tyrosine kinase inhibitor, cancer autoimmune disease treatment fused pyrimidine btk inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

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

On March 24, 2022, Zhao, Hong-Yi; Wang, Hai-Peng; Mao, Yu-Ze; Zhang, Hao; Xin, Minhang; Xi, Xiao-Xiao; Lei, Hao; Mao, Shuai; Li, Dong-Hui; Zhang, San-Qi published an article.SDS of cas: 16230-24-3 The title of the article was Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. And the article contained the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFRL858R/T790M and EGFRdel19, reaching the lowest DC50 values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFRL858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).SDS of cas: 16230-24-3

The Article related to pyrimidine preparation antitumor egfr inhibition sar mol docking, purine preparation antitumor egfr inhibition sar mol docking, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 16230-24-3

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