Month: December 2021

In 2020.0 ORG PROCESS RES DEV published article about HYDROGEN; BROMIDES; OLEFINS; ARYL in [Kallemeyn, Jeffrey M.; Engstrom, Kenneth M.; Pelc, Matthew J.; Lukin, Kirill A.; Morrill, Westin H.; Wei, Haojuan; Towne, Timothy B.; Henle, Jeremy; Nere, Nandkishor K.; Welch, Dennie S.; Shekhar, Shashank; Ravn, Matthew M.; Zhao, Gang; Fickes, Michael G.; Cink, Russell D.] AbbVie Inc, Proc Res & Dev, N Chicago, IL 60064 USA; [Ding, Chen; Vinci, John C.; Marren, James] AbbVie Inc, Analyt Res & Dev, N Chicago, IL 60064 USA in 2020.0, Cited 35.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9. Recommanded Product: 91-00-9

Glecaprevir was identified as a potent hepatitis C virus (HCV) protease inhibitor, and a large-scale synthesis was required to support the late-stage clinical trials and subsequent commercial launch. The large-scale synthetic route to glecaprevir required the development of completely new synthetic approaches to the two key structural features: the 18-membered macrocycle 3 and the difluoromethyl-substituted cyclopropyl amino acid 4. In this first manuscript, we describe the route development for the macrocycle 3; the second manuscript will describe the development of a new synthetic route to the difluoromethyl-substituted cyclopropyl amino acid 4 and the final assembly of glecaprevir. The large-scale synthetic route to the macrocycle employed a unique intramolecular etherification reaction as the key step in the macrocycle synthesis, avoiding the scalability limitations of the ring-closing metathesis (RCM) reaction of the enabling route. The large-scale synthetic route to the macrocycle was successfully used to produce the amount of glecaprevir required to support the late-stage clinical development.

Recommanded Product: 91-00-9. About Diphenylmethanamine, If you have any questions, you can contact Kallemeyn, JM; Engstrom, KM; Pelc, MJ; Lukin, KA; Morrill, WH; Wei, HJ; Towne, TB; Henle, J; Nere, NK; Welch, DS; Shekhar, S; Ravn, MM; Zhao, G; Fickes, MG; Ding, C; Vinci, JC; Marren, J; Cink, RD or concate me.

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

An article Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one containing 4,5-dihydrothiazole-2-thiol derivatives against Meloidogyne incognita WOS:000485554100001 published article about ANTICANCER; DISCOVERY; LARGAZOLE in [Chen, Xiulei; Zhou, Zhen; Li, Zhong; Xu, Xiaoyong] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China; [Li, Zhong; Xu, Xiaoyong] Shanghai Collaborat Innovat Ctr Biomfg Technol, Shanghai, Peoples R China in 2020, Cited 29. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4. HPLC of Formula: C7H5N3O

A series of novel 1,2,3-benzotriazin-4-one derivatives containing 4,5-dihydrothiazole-2-thiol were synthesized and characterized by H-1 NMR, C-13 NMR, F-19 NMR and HRMS. The bioassay results showed that compounds 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-7-methoxybenzo[d][1-3]triazin-4(3H)-one, 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-6-nitrobenzo[d][1-3]triazin-4(3H)-one, 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1-3]triazin-4(3H)-one exhibited good control efficacy against the cucumber root-knot nematode disease caused by Meloidogyne incognita at the concentration of 10.0 mg L-1 in vivo. Compound 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1-3]triazin-4(3H)-one showed excellent nematicidal activity with inhibition 68.3% at a concentration of 1.0 mg L-1. It suggested that the structure of 1,2,3-benzotriazin-4-one containing 4,5-dihydro-thiazole-2-thiol could be optimized further.

HPLC of Formula: C7H5N3O. Welcome to talk about 90-16-4, If you have any questions, you can contact Chen, XL; Zhou, Z; Li, Z; Xu, XY or send Email.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Quality Control of Benzo[d][1,2,3]triazin-4(3H)-one. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM) published in 2019, Reprint Addresses Pal, M (corresponding author), Dr Reddys Inst Life Sci, Univ Hyderabad Campus, Hyderabad 500046, India.. The CAS is 90-16-4. Through research, I have a further understanding and discovery of Benzo[d][1,2,3]triazin-4(3H)-one.

The chorismate mutase (CM) is considered as an attractive target for the identification of potential antitubercular agents due to its absence in animals but not in bacteria. A series of 3-indolylmethyl substituted pyrazolo-triazinone derivatives were designed and docked into CM in silico as potential inhibitors. These compounds were efficiently synthesized using the Pd/Cu-catalyzed coupling-cyclization in a single pot involving the construction of indole ring. The methodology was later extended to the preparation of corresponding benzo analogs of pyrazolotriazinones i.e. 3-indolylmethyl substituted benzotriazinone derivatives. Several of these novel compounds showed significant inhibition of CM when tested in vitro at 30 mu M. The SAR (Structure-Activity-Relationship) studies suggested that benzotriazinone moiety was more favorable over the pyrazolotriazinone ring. The two best active compounds showed IC50 similar to 0.4-0.9 mu M (better than the reference/known compounds used) and no toxicity till 30 mu M in vitro.

Quality Control of Benzo[d][1,2,3]triazin-4(3H)-one. Welcome to talk about 90-16-4, If you have any questions, you can contact Reddy, GS; Snehalatha, AV; Edwin, RK; Hossain, KA; Giliyaru, VB; Hariharapura, RC; Shenoy, GG; Misra, P; Pal, M or send Email.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recently I am researching about PROLIFERATOR-ACTIVATED RECEPTORS; GAMMA MODULATOR; FATTY-ACIDS; BINDING; IDENTIFICATION, Saw an article supported by the Japan Society for the Promotion of Science [KAKENHI]Ministry of Education, Culture, Sports, Science and Technology, Japan (MEXT)Japan Society for the Promotion of ScienceGrants-in-Aid for Scientific Research (KAKENHI) [17K13264]. Published in MDPI in BASEL ,Authors: Utsugi, Y; Kobuchi, H; Kawamura, Y; Atito, ASA; Nagao, M; Isoda, H; Miyamae, Y. The CAS is 104-10-9. Through research, I have a further understanding and discovery of 2-(4-Aminophenyl)ethanol. Recommanded Product: 104-10-9

Covalent agonists of PPAR cause unique receptor conformational changes and behave as selective PPAR modulators, whereas there are few covalent agonists other than endogenous unsaturated fatty acids metabolites. Previously, we established a cell-based strategy to identify new PPAR ligands and synthesized a new-type of covalent agonist that possesses the hybrid structure of a plant-derived cinnamic acid derivative and GW9662, a covalent antagonist. Herein, we report six analogues that differ in how the two fragments are linked together. Compounds with a simplified linker showed potent agonistic activity with improved EC50 values (less than 5 nM), indicating that close proximity between the two fragments improves binding affinity. When the position of cinnamic acid moiety was placed at 4 carbon of aniline ring, PPAR agonist activity was completely abolished. Docking studies suggested that the activation profile likely depends on interaction with the cavity around helix 3, -sheet, and -loop region in the ligand-binding domain. Furthermore, a cell-based assay revealed that agonist-type compounds activate PPAR transcription in a manner dependent on covalent linkage with the Cys285 residue leading to prolonged transactivation. This activation feature reflects pharmacological benefits of covalent drugs, suggesting that these hybrid compounds may serve as potential leads for a new-class of covalent PPAR ligands.

Welcome to talk about 104-10-9, If you have any questions, you can contact Utsugi, Y; Kobuchi, H; Kawamura, Y; Atito, ASA; Nagao, M; Isoda, H; Miyamae, Y or send Email.. Recommanded Product: 104-10-9

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

In 2020 TETRAHEDRON LETT published article about ALLYLIC SUBSTITUTION; FUNCTIONALIZATION; HYDROAMINATION; HETEROCYCLES; 2-PYRIDONES; ALKYLATION; DISCOVERY in [Zhang, Zhiguang; Dai, Siwei; Li, Ling; Jia, Chenyu; Zhang, Yong] Hebei Univ Sci & Technol, Coll Chem & Pharmaceut Engn, 26 Yuxiang Rd, Shijiazhuang 050018, Hebei, Peoples R China; [Li, Hao] East China Univ Sci & Technol, State Key Lab Bioengn Reactor, Shanghai Key Lab New Drug Design, 130 Meilong Rd, Shanghai 200237, Peoples R China; [Li, Hao] East China Univ Sci & Technol, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China in 2020, Cited 35. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4. COA of Formula: C7H5N3O

We described a novel scandium-catalyzed selective Michael addition of quinazolinones and vinylazaarenes. The protocol proceeds smoothly to give diverse quinazolinone derivatives in moderate to excellent yields. The high practicality of this protocol was proved by excellent chemo selectivity and broad substrate and functional group compatibility. (C) 2020 Elsevier Ltd. All rights reserved.

Bye, fridends, I hope you can learn more about C7H5N3O, If you have any questions, you can browse other blog as well. See you lster.. COA of Formula: C7H5N3O

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recently I am researching about CATALYZED DENITROGENATIVE ANNULATION; TERT-BUTYL NITRITE; NEMATOCIDAL ACTIVITIES; SELECTIVE SYNTHESIS; DERIVATIVES; 1,2,3-BENZOTRIAZINE-4-(3H)-ONES; ACID, Saw an article supported by the Council of Scientific and Industrial Research, New DelhiCouncil of Scientific & Industrial Research (CSIR) – India [BSC-0114]. COA of Formula: C7H5N3O. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Barak, DS; Mukhopadhyay, S; Dahatonde, DJ; Batra, S. The CAS is 90-16-4. Through research, I have a further understanding and discovery of Benzo[d][1,2,3]triazin-4(3H)-one

An efficient transformation of 2-aminobenzamides to 1,2,3-benzotriazin-4(3H)-ones in the presence of sodium nitrite (NaNO2) and Iodine (I-2) is described. The reaction is proposed to proceed via formation of nitrosyl halide that induces nitrosylation of the amino group of 2-aminobenzamide leading to diazotization followed by intramolecular cyclization. (C) 2018 Elsevier Ltd. All rights reserved.

COA of Formula: C7H5N3O. Bye, fridends, I hope you can learn more about C7H5N3O, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

An article Gas-separation and physical properties of ABA triblock copolymers synthesized from polyimide and hydrophilic adamantane derivatives WOS:000566926500020 published article about AROMATIC POLYAMIDES; MEMBRANES; POLYMERS; CAPTURE in [Ito, Tsubasa; Shiota, Ryunosuke; Taniguchi, Naomi; Nagai, Kazukiyo] Meiji Univ, Dept Appl Chem, Tama Ku, 1-1-1 Higashi Mita, Kawasaki, Kanagawa 2148571, Japan; [Spontak, Richard J.] North Carolina State Univ, Dept Chem & Biomol Engn, Raleigh, NC 27695 USA; [Spontak, Richard J.] North Carolina State Univ, Dept Mat Sci & Engn, Raleigh, NC 27695 USA in 2020.0, Cited 44.0. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9. COA of Formula: C8H11NO

In this study, ABA triblock copolymers derived from 4,4′-(hexafluoroisopropylidene)-diphthalic anhydride-2,3,5,6-tetramethyl-1,4-phenylenediamine (6FDA-TeMPD; PI) and 3-hydroxy-1-adamantyl methacrylate (HAdMA) or 3,5-dihydroxy-1-adamantyl methacrylate (DHAdMA) have been synthesized via atom transfer radical polymerization to generate mechanically tough and thermally stable gas-separation membranes with composition-tunable transport properties. Due to the inherent thermodynamic incompatibility between the chemically dissimilar blocks, these two series of triblock copolymers appear microphase-separated. While the gas permeability coefficients of these triblock copolymer membranes are consistently lower than that of PI due to the reduced fractional free volume of HAdMA and DHAdMA, the solubility coefficients of the copolymers are higher than that of PI due presumably to specific interactions between the polar hydroxyl group(s) and penetrant gas molecules. These triblock copolymers synthesized from PI and hydrophilic adamantane derivatives constitute a new class of nanostructured polymeric materials possessing excellent thermomechanical properties in conjunction with designer gas-separation properties.

Welcome to talk about 104-10-9, If you have any questions, you can contact Ito, T; Shiota, R; Taniguchi, N; Spontak, RJ; Nagai, K or send Email.. COA of Formula: C8H11NO

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

HPLC of Formula: C13H13N. Recently I am researching about SUFEX CLICK CHEMISTRY; NUCLEOPHILIC-SUBSTITUTION; N-ALKYLATION; SULFONAMIDES; ARYL; DISCOVERY; AMINES; ARYLATION; PEPTIDES; REAGENTS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21502241]; Natural Science Foundation of Guangdong ProvinceNational Natural Science Foundation of Guangdong Province [2016A030313290]. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87-99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.

HPLC of Formula: C13H13N. Welcome to talk about 91-00-9, If you have any questions, you can contact Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L or send Email.

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

An article Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM) WOS:000487812000051 published article about 1,2,3-BENZOTRIAZIN-4-ONE DERIVATIVES; NEMATOCIDAL ACTIVITIES; INDOLES; 1-ALKYNES; RV1885C; 2-HETEROARYL; DOCKING; PROTEIN; 2-ARYL in [Reddy, Gangireddy Sujeevan; Snehalatha, Ampalam Venkata; Edwin, Rebecca Kristina; Hossain, Kazi Amirul; Misra, Parimal; Pal, Manojit] Dr Reddys Inst Life Sci, Univ Hyderabad Campus, Hyderabad 500046, India; [Reddy, Gangireddy Sujeevan; Giliyaru, Varadaraj Bhat; Hariharapura, Raghu Chandrashekhar; Shenoy, G. Gautham] Manipal Acad Higher Educ, Manipal Coll Pharmaceut Sci, Manipal 576104, Karnataka, India in 2019, Cited 38. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4. Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one

The chorismate mutase (CM) is considered as an attractive target for the identification of potential antitubercular agents due to its absence in animals but not in bacteria. A series of 3-indolylmethyl substituted pyrazolo-triazinone derivatives were designed and docked into CM in silico as potential inhibitors. These compounds were efficiently synthesized using the Pd/Cu-catalyzed coupling-cyclization in a single pot involving the construction of indole ring. The methodology was later extended to the preparation of corresponding benzo analogs of pyrazolotriazinones i.e. 3-indolylmethyl substituted benzotriazinone derivatives. Several of these novel compounds showed significant inhibition of CM when tested in vitro at 30 mu M. The SAR (Structure-Activity-Relationship) studies suggested that benzotriazinone moiety was more favorable over the pyrazolotriazinone ring. The two best active compounds showed IC50 similar to 0.4-0.9 mu M (better than the reference/known compounds used) and no toxicity till 30 mu M in vitro.

Welcome to talk about 90-16-4, If you have any questions, you can contact Reddy, GS; Snehalatha, AV; Edwin, RK; Hossain, KA; Giliyaru, VB; Hariharapura, RC; Shenoy, GG; Misra, P; Pal, M or send Email.. Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

An article Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections WOS:000466053900012 published article about DIHYDROFOLATE-REDUCTASE; THYMIDYLATE SYNTHASE; BINDING MODES; LEISHMANIA; IDENTIFICATION; ASSAY; DERIVATIVES; VALIDATION; SOLUBILITY; RESISTANCE in [Linciano, Pasquale; Luciani, Rosaria; Sesenna, Antony; Quotadamo, Antonio; Costantino, Luca; Costi, Maria Paola] Univ Modena & Reggio Emilia, Dipartimento Sci Vita, Via Campi 103, I-41125 Modena, Italy; [Pozzi, Cecilia; dello Iacono, Lucia; di Pisa, Flavio; Landi, Giacomo; Bonucci, Alessio; Mangani, Stefano] Univ Siena, Dipartimento Biotecnol Chim & Farm, Via Aldo Moro 2, I-53100 Siena, Italy; [Gul, Sheraz; Kuzikov, Maria; Ellinger, Bernhard; Witt, Gesa] Fraunhofer Inst Mol Biol & Appl Ecol Screening Po, D-22525 Hamburg, Germany; [Santarem, Nuno; Baptista, Catarina] Inst Mol & Cell Biol, P-4150180 Porto, Portugal; [Santarem, Nuno; Baptista, Catarina] Univ Porto, Inst Invest & Inovacao Saude, P-4150180 Porto, Portugal; [Franco, Caio; Moraes, Carolina B.] CNPEM, Lab Nacl Biociencias LNBio, BR-13083100 Campinas, SP, Brazil; [Mueller, Wolfgang; Wittig, Ulrike] HITS, Sci Databases & Visualizat Grp, D-69118 Heidelberg, Germany; [Wittig, Ulrike] HITS, Mol & Cellular Modeling Grp, D-69118 Heidelberg, Germany; [Franco, Caio; Moraes, Carolina B.] Univ Sao Paulo, Dept Microbiol, Inst Biomed Sci, BR-05508900 Sao Paulo, SP, Brazil in 2019.0, Cited 57.0. Name: Diphenylmethanamine. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

2-Amino-benzo[d]thiazole was identified as a new scaffold for the development of improved pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic agents. Molecular docking and crystallography guided the design and synthesis of 42 new benzothiazoles. The compounds were assessed for Trypanosoma brucei and Leishmania major PTR1 inhibition and in vitro activity against T. brucei and amastigote Leishmania infantum. We identified several 2-amino-benzo[d]thiazoles with improved enzymatic activity (TbPTR1 IC50 = 0.35 mu M; LmPTR1 IC50 = 1.9 mu M) and low mu M antiparasitic activity against T. brucei. The ten most active compounds against TbPTR1 were able to potentiate the antiparasitic activity of methotrexate when evaluated in combination against T. brucei, with a potentiating index between 1.2 and 2.7. The compound library was profiled for early ADME toxicity, and 2-amino-N-benzylbenzo[d]thiazole-6-carboxamide (4c) was finally identified as a novel potent, safe, and selective anti-trypanocydal agent (EC50 = 7.0 mu M). Formulation of 4c with hydroxypropyl-beta-cyclodextrin yielded good oral bioavailability, encouraging progression to in vivo studies.

Welcome to talk about 91-00-9, If you have any questions, you can contact Linciano, P; Pozzi, C; dello Iacono, L; di Pisa, F; Landi, G; Bonucci, A; Gul, S; Kuzikov, M; Ellinger, B; Witt, G; Santarem, N; Baptista, C; Franco, C; Moraes, CB; Muller, W; Wittig, U; Luciani, R; Sesenna, A; Quotadamo, A; Ferrari, S; Pohner, I; Cordeiro-Da-Silva, A; Mangani, S; Costantino, L; Costi, MP or send Email.. Name: Diphenylmethanamine

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