Day: October 25, 2021

Category: isothiazole. Authors Lin, TT; Li, JC; Liu, LP; Li, YQ; Jiang, HL; Chen, KX; Xu, P; Luo, C; Zhou, B in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about in [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 200031, Peoples R China; [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Xu, Pan; Luo, Cheng] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Chem Biol,Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Zhou, Bing] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng; Zhou, Bing] Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China in 2021, Cited 39. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

Cyclin-dependent kinases play significant roles in cell cycle progression and are promising targets for cancer therapy. However, most potent CDK inhibitors lack the balance between efficacy and safety because of poor selectivity. Given the roles of CDK2 in tumorigenesis, selective CDK2 inhibition may provide therapeutic benefits against certain cancer. In this study, a series of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives were designed, synthesized, and evaluated. The most selective compound DC-K2in212 in this series exhibited high potency towards CDK2 and had effective anti-proliferative activity against A2058 melanoma cell line and MV4-11 leukemia cell line while exhibiting low toxic effect on human normal cell lines MRC5 and LX2. The molecular modeling illustrated that compound DC-K2in212 had the similar binding mode with CDK2 as C-73, the most selective CDK2 inhibitor reported so far, which might account for selectivity against CDK2 over CDK1. Further biological studies revealed that compound DC-K2in212 suppressed CDK2-associated downstream signaling pathway, blocked cell cycle progression, and induced cellular apoptosis. Therefore, compound DC-K2in212 could serve as a potential CDK2 inhibitor for further development. (c) 2021 Elsevier Masson SAS. All rights reserved.

About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Lin, TT; Li, JC; Liu, LP; Li, YQ; Jiang, HL; Chen, KX; Xu, P; Luo, C; Zhou, B or concate me.. Category: isothiazole

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Matsushita, T; Sati, GC; Kondasinghe, N; Pirrone, MG; Kato, T; Waduge, P; Kumar, HS; Sanchon, AC; Dobosz-Bartoszek, M; Shcherbakov, D; Juhas, M; Hobbie, SN; Schrepfer, T; Chow, CS; Polikanov, YS; Schacht, J; Vasella, A; Bottger, EC; Crich, D in [Matsushita, Takahiko; Sati, Girish C.; Kondasinghe, Nuwan; Pirrone, Michael G.; Kato, Takayuki; Waduge, Prabuddha; Chow, Christine S.; Crich, David] Wayne State Univ, Dept Chem, 5101 Cass Ave, Detroit, MI 48202 USA; [Kumar, Harshitha Santhosh; Sanchon, Adrian Cortes; Shcherbakov, Dimitri; Juhas, Mario; Hobbie, Sven N.; Bottger, Erik C.] Univ Zurich, Inst Med Mikrobiol, 28 Gloriastr, CH-8006 Zurich, Switzerland; [Dobosz-Bartoszek, Malgorzata; Polikanov, Yury S.] Univ Illinois, Dept Biol Sci, 900 South Ashland Ave, Chicago, IL 60607 USA; [Schrepfer, Thomas; Schacht, Jochen] Univ Michigan, Kresge Hearing Res Inst, Dept Otolaryngol, 1150 West Med Ctr Dr, Ann Arbor, MI 48109 USA; [Polikanov, Yury S.] Univ Illinois, Dept Med Chem & Pharmacognosy, 900 South Ashland Ave, Chicago, IL 60607 USA; [Vasella, Andrea] Swiss Fed Inst Technol, Lab Organ Chem, Vladimir Prelog Weg 1-5-10, CH-8093 Zurich, Switzerland published Design, Multigram Synthesis, and in Vitro and in Vivo Evaluation of Propylamycin: A Semisynthetic 4,5-Deoxystreptamine Class Aminoglycoside for the Treatment of Drug-Resistant Enterobacteriaceae and Other Gram-Negative Pathogens in 2019, Cited 56. COA of Formula: C14H10O3. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0.

Infectious diseases due to multidrug-resistant pathogens, particularly carbapenem-resistant Enterobacteriaceae (CREs), present a major and growing threat to human health and society, providing an urgent need for the development of improved potent antibiotics for their treatment. We describe the design and development of a new class of aminoglycoside antibiotics culminating in the discovery of propylamycin. Propylamycin is a 4′-deoxy-4′-alkyl paromomycin whose alkyl substituent conveys excellent activity against a broad spectrum of ESKAPE pathogens and other Gram-negative infections, including CREs, in the presence of numerous common resistance determinants, be they aminoglycoside modifying enzymes or rRNA methyl transferases. Importantly, propylamycin is demonstrated not to be susceptible to the action of the ArmA resistance determinant whose presence severely compromises the action of plazomicin and all other 4,6-disubstituted 2-deoxystreptamine aminoglycosides. The lack of susceptibility to ArmA, which is frequently encoded on the same plasmid as carbapenemase genes, ensures that propylamycin will not suffer from problems of cross-resistance when used in combination with carbapenems. Cell-free translation assays, quantitative ribosome footprinting, and X-ray crystallography support a model in which propylamycin functions by interference with bacterial protein synthesis. Cell-free translation assays with humanized bacterial ribosomes were used to optimize the selectivity of propylamycin, resulting in reduced ototoxicity in guinea pigs. In mouse thigh and septicemia models of Escherichia coli, propylamycin shows excellent efficacy, which is better than paromomycin. Overall, a simple novel deoxy alkyl modification of a readily available aminoglycoside antibiotic increases the inherent antibacterial activity, effectively combats multiple mechanisms of aminoglycoside resistance, and minimizes one of the major side effects of aminoglycoside therapy.

COA of Formula: C14H10O3. About Benzoic anhydride, If you have any questions, you can contact Matsushita, T; Sati, GC; Kondasinghe, N; Pirrone, MG; Kato, T; Waduge, P; Kumar, HS; Sanchon, AC; Dobosz-Bartoszek, M; Shcherbakov, D; Juhas, M; Hobbie, SN; Schrepfer, T; Chow, CS; Polikanov, YS; Schacht, J; Vasella, A; Bottger, EC; Crich, D or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2020 ADV SYNTH CATAL published article about ENANTIOSELECTIVE SYNTHESIS; PHOSPHORUS LIGANDS; BRONSTED ACID; ALCOHOLS; ACTIVATION; BATCH; CATALYSIS; SECONDARY in [Lai, Junshan; Pericas, Miquel A.] Barcelona Inst Sci & Technol, Inst Chem Res Catalonia ICIQ, Av Paisos Catalans 16, Tarragona 43007, Spain; [Lai, Junshan] Univ Rovira & Virgili, Dept Quim Analit & Quim Organ, E-43007 Tarragona, Spain; [Neyyappadath, Rifahath M.; Smith, Andrew D.] Univ St Andrews, Sch Chem, EaStCHEM, St Andrews KY16 9ST, Fife, Scotland; [Pericas, Miquel A.] Univ Barcelona, Dept Quim Inorgan & Organ, E-08028 Barcelona, Spain in 2020, Cited 47. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Recommanded Product: Benzoic anhydride

A polystyrene-immobilized isothiourea has been applied to the enantioselective acylative kinetic resolution (KR) of monoacylated BINOL(s) with inexpensive isobutyric anhydride in batch and flow. High selectivity values (s=29 at 0 degrees C) and a remarkable stability of the catalytic system in the operation conditions have been recorded for unsubstituted BINOL. No significant loss of activity/selectivity is recorded after 10 consecutive KR cycles in batch. A continuous flow process has been implemented and operated with a 100 mmol (32.8 g) sample of racemic monoacetylated BINOL in dichloromethane solution in an 84 hours experiment with a packed bed reactor containing 1 g (f=0.37 mmol.g(-1)) of the functional resin (s=17-21). Residence time can be decreased to 10 min with the same reactor to achieve a conversion of 58% with a selectivity factor s=17 when a more highly functionalized catalyst (f=0.88 mmol.g(-1)) is used. This translates into a remarkable combined productivity of 5.5 mmol(prod) . mmol(cat)(-1) . h(-1).

Recommanded Product: Benzoic anhydride. About Benzoic anhydride, If you have any questions, you can contact Lai, JS; Neyyappadath, RM; Smith, AD; Pericas, MA or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Asymmetric Synthesis of Adjacent Tri- and Tetrasubstituted Carbon Stereocenters: Organocatalytic Aldol Reaction of an Hydantoin Surrogate with Azaarene 2-Carbaldehydes WOS:000484834700001 published article about CATALYTIC ENANTIOSELECTIVE SYNTHESIS; HETERO-DIELS-ALDER; CONJUGATE ADDITION; N-OXIDES; QUATERNARY STEREOCENTERS; MANNICH REACTIONS; MUKAIYAMA-ALDOL; DERIVATIVES; PYRIDINE; CONSTRUCTION in [Izquierdo, June; Demurget, Noemie; Landa, Aitor; Oiarbide, Mikel; Palomo, Claudio] Univ Basque Country, Dept Quim Organ 1, UPV EHU, Manuel Lardizabal 3, San Sebastian 20018, Spain; [Brinck, Tore; Diner, Peter] KTH Royal Inst Technol, Dept Chem, Tekn Ringen 30, S-10044 Stockholm, Sweden; [Mercero, Jose M.] Euskal Herriko Unibertsitatea, Kimika Fak, UPV EHU, Donostia San Sebastian, Spain; [Mercero, Jose M.] Donostia Int Phys Ctr DIPC, Donostia San Sebastian, Spain in 2019, Cited 122. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. HPLC of Formula: C14H10O3

A bifunctional amine/squaramide catalyst promoted direct aldol addition of an hydantoin surrogate to pyridine 2-carbaldehyde N-oxides to afford adducts bearing two vicinal tertiary/quaternary carbons in high diastereo- and enantioselectivity (d.r. up to >20:1; ee up to 98 %) is reported. Acid hydrolysis of adducts followed by reduction of the N-oxide group yields enantiopure carbinol-tethered quaternary hydantoin-azaarene conjugates with densely functionalized skeletons. DFT studies of the potential energy surface (B3LYP/6-31+G(d)+CPCM (dichloromethane)) of the reaction correlate the activity of different catalysts and support an intramolecular hydrogen-bond-assisted activation of the squaramide moiety in the transition state of the catalytic reaction.

About Benzoic anhydride, If you have any questions, you can contact Izquierdo, J; Demurget, N; Landa, A; Brinck, T; Mercero, JM; Diner, P; Oiarbide, M; Palomo, C or concate me.. HPLC of Formula: C14H10O3

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

HPLC of Formula: C8H8O2. Recently I am researching about ONE-STEP SYNTHESIS; ONE-POT SYNTHESIS; N-C CLEAVAGE; ORGANOMETALLIC REAGENTS; EFFICIENT SYNTHESIS; CATALYZED SYNTHESIS; DIRECT CONVERSION; ACID-DERIVATIVES; CARBON-MONOXIDE; ACYL CHLORIDES, Saw an article supported by the Knut and Alice Wallenberg FoundationKnut & Alice Wallenberg Foundation [KAW2016.0153]; European Research CouncilEuropean Research Council (ERC)European Commission [714737]; Department of Organic Chemistry at Stockholm University. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Colas, K; dos Santos, ACVD; Mendoza, A. The CAS is 99-04-7. Through research, I have a further understanding and discovery of 3-Methylbenzoic acid

The direct preparation of ketones from carboxylate anions is greatly limited by the required use of organolithium reagents or activated acyl sources that need to be independently prepared. Herein, a specific magnesium amide additive is used to activate and control the addition of more tolerant Grignard reagents to carboxylate anions. This strategy enables the modular synthesis of ketones from CO2 and the preparation of isotopically labeled pharmaceutical building blocks in a single operation.

HPLC of Formula: C8H8O2. About 3-Methylbenzoic acid, If you have any questions, you can contact Colas, K; dos Santos, ACVD; Mendoza, A or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2019.0 J AM CHEM SOC published article about H REDUCTIVE ELIMINATION; C-H; OXIDATION LEVEL; ARYL BROMIDES; CARBONYL ALLYLATION; AROMATIC-ALDEHYDES; O-H; ENANTIOSELECTIVE ADDITION; DIRECT ACYLATION; ORGANIC HALIDES in [Swyka, Robert A.; Zhang, Wandi; Krische, Michael J.] Univ Texas Austin, Dept Chem, Austin, TX 78712 USA; [Richardson, Jeffery] Eli Lilly & Co Ltd, Discovery Chem Res & Technol, Windlesham GU20 6PH, Surrey, England; [Ruble, J. Craig] Eli Lilly & Co, Discovery Chem Res & Technol, Indianapolis, IN 46285 USA in 2019.0, Cited 82.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Safety of 2,5-Dimethoxybenzaldehyde

The first intermolecular carbonyl arylations via transfer hydrogenative reductive coupling are described. Using rhodium catalysts modified by (Bu2PMe)-Bu-t, sodium formate-mediated reductive coupling of aryl iodides with aldehydes occurs in a chemoselective fashion in the presence of protic functional groups and lower halides. This work expands the emerging paradigm of transfer hydrogenative coupling as an alternative to preformed carbanions or metallic reductants in C=X addition.

Safety of 2,5-Dimethoxybenzaldehyde. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Swyka, RA; Zhang, WD; Richardson, J; Ruble, JC; Krische, MJ or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article NBS-activated cross-dehydrogenative esterification of carboxylic acids with DMSO WOS:000569870300014 published article about O BOND FORMATION; C-H LACTONIZATION; DIMETHYL-SULFOXIDE; CATALYZED C(SP(2))-H; EXPEDIENT SYNTHESIS; PUMMERER REACTION; METHYL KETONES; FACILE ACCESS; STRATEGY; FUNCTIONALIZATION in [Wu, Ya; Zhang, Mengsha; Zhang, Yanli; Li, Mingyang; Feng, Weisheng; Zheng, Xiaoke] Henan Univ Chinese Med, Sch Pharm, Zhengzhou 450046, Henan, Peoples R China; [Wu, Ya; Zhang, Mengsha; Zhang, Yanli; Li, Mingyang; Feng, Weisheng; Zheng, Xiaoke] Henan Univ Chinese Med, Collaborat Innovat Ctr Resp Dis Diag & Treatment, Zhengzhou 450046, Henan, Peoples R China; [Tang, Lin] Xinyang Normal Univ, Coll Chem & Chem Engn, Xinyang 464000, Henan, Peoples R China in 2020, Cited 75. The Name is 3-Methylbenzoic acid. Through research, I have a further understanding and discovery of 99-04-7. Formula: C8H8O2

The firstN-bromosuccinimide (NBS)-promoted transition metal-free cross-dehydrogenative esterification of carboxylic acids with dimethyl sulfoxide (DMSO) has been disclosed for formal C-O formationviaPummerer-type rearrangement. These transformations employ readily available carboxylic acids as the nucleophile and DMSO as the sulfur-containing carbon source and solvent under mild conditions, affording valuable (methylsulfinyl)methyl esters with a broad substrate scope. Furthermore, the developed protocol provides an efficient and straightforward method for the preparation of deuterated (methylsulfinyl)methyl esters by use of deuterium-labelled DMSO as the reagent.

About 3-Methylbenzoic acid, If you have any questions, you can contact Wu, Y; Zhang, MS; Zhang, YL; Li, MY; Feng, WS; Zheng, XK; Tang, L or concate me.. Formula: C8H8O2

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Continuous Flow Preparation of Enantiomerically Pure BINOL(s) by Acylative Kinetic Resolution WOS:000509518500001 published article about ENANTIOSELECTIVE SYNTHESIS; PHOSPHORUS LIGANDS; BRONSTED ACID; ALCOHOLS; ACTIVATION; BATCH; CATALYSIS; SECONDARY in [Lai, Junshan; Pericas, Miquel A.] Barcelona Inst Sci & Technol, Inst Chem Res Catalonia ICIQ, Av Paisos Catalans 16, Tarragona 43007, Spain; [Lai, Junshan] Univ Rovira & Virgili, Dept Quim Analit & Quim Organ, E-43007 Tarragona, Spain; [Neyyappadath, Rifahath M.; Smith, Andrew D.] Univ St Andrews, Sch Chem, EaStCHEM, St Andrews KY16 9ST, Fife, Scotland; [Pericas, Miquel A.] Univ Barcelona, Dept Quim Inorgan & Organ, E-08028 Barcelona, Spain in 2020, Cited 47. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. COA of Formula: C14H10O3

A polystyrene-immobilized isothiourea has been applied to the enantioselective acylative kinetic resolution (KR) of monoacylated BINOL(s) with inexpensive isobutyric anhydride in batch and flow. High selectivity values (s=29 at 0 degrees C) and a remarkable stability of the catalytic system in the operation conditions have been recorded for unsubstituted BINOL. No significant loss of activity/selectivity is recorded after 10 consecutive KR cycles in batch. A continuous flow process has been implemented and operated with a 100 mmol (32.8 g) sample of racemic monoacetylated BINOL in dichloromethane solution in an 84 hours experiment with a packed bed reactor containing 1 g (f=0.37 mmol.g(-1)) of the functional resin (s=17-21). Residence time can be decreased to 10 min with the same reactor to achieve a conversion of 58% with a selectivity factor s=17 when a more highly functionalized catalyst (f=0.88 mmol.g(-1)) is used. This translates into a remarkable combined productivity of 5.5 mmol(prod) . mmol(cat)(-1) . h(-1).

COA of Formula: C14H10O3. About Benzoic anhydride, If you have any questions, you can contact Lai, JS; Neyyappadath, RM; Smith, AD; Pericas, MA or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Hirose, Y; Yamazaki, M; Nogata, M; Nakamura, A; Maegawa, T in [Hirose, Yuuka; Yamazaki, Mirai; Nogata, Misa; Nakamura, Akira; Maegawa, Tomohiro] Kindai Univ, Sch Pharmaceut Sci, Osaka 5778502, Japan published Aromatic Halogenation Using N-Halosuccinimide and PhSSiMe3 or PhSSPh in 2019, Cited 43. Name: 1,3-Dimethoxybenzene. The Name is 1,3-Dimethoxybenzene. Through research, I have a further understanding and discovery of 151-10-0.

We developed a mild aromatic halogenation reaction using a combination of N-halosuccinimide and PhSSiMe3 or PhSSPh. Less reactive aromatic compounds, such as methyl 4-methoxybenzoate, were brominated with PhSSiMe3 or PhSSPh and N-bromosuccinimide in high yields. No reaction was observed in the absence of PhSSiMe3 or PhSSPh. This method is also applicable to chlorination reactions using N-chlorosuccinimide and PhSSPh.

Name: 1,3-Dimethoxybenzene. About 1,3-Dimethoxybenzene, If you have any questions, you can contact Hirose, Y; Yamazaki, M; Nogata, M; Nakamura, A; Maegawa, T or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Rh(II)-Catalyzed C-H Alkylation of Benzylamines with Unactivated Alkenes: The Influence of Acid on Linear and Branch Selectivity WOS:000661126700036 published article about AROMATIC AMIDES; CATALYZED ALKYLATION; BONDS; DERIVATIVES in [Das, Amrita; Chatani, Naoto] Osaka Univ, Fac Engn, Dept Appl Chem, Suita, Osaka 5650871, Japan in 2021, Cited 47. Computed Properties of C7H4F2O2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2

The Rh-catalyzed C-H alkylation of benzylamine derivatives with unactivated 1-alkenes that proceeds via a picolinamide directing group is reported. The crucial role of an acid additive in this transformation is confirmed. Aromatic acids showed high linear selectivity, and aliphatic acids provided branched alkylation products as the major product. The reaction has a broad scope for benzylamines and alkenes. Deuterium labeling experiments suggest that a Rh-carbene intermediate is involved in the case of linear product formation. A different reaction pathway, however, appears to be involved in the case of branched alkylation products, and this pathway also appeared to be a minor pathway in linear-selective reactions.

Computed Properties of C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact Das, A; Chatani, N or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com