Day: October 17, 2022

Tan, Guangying; Das, Mowpriya; Maisuls, Ivan; Strassert, Cristian A.; Glorius, Frank published the artcile< Rhodium-Catalyzed Dealkenylative Arylation of Alkenes with Arylboronic Compounds>, Synthetic Route of 13788-92-6, the main research area is biaryl preparation; alkene arylboronic compound dealkenylative arylation rhodium catalyst; C−C bond cleavage; alkenes; dealkenylation arylation; organic fluorescent molecules; rhodium catalysis.

Herein, the first example of rhodium-catalyzed dealkenylative arylation of alkenes with arylboronic compounds, thereby providing an unconventional access to biaryls with excellent chemoselectivity was diclosed. In this method, C(aryl)-C(alkenyl) and C(alkenyl)-C(alkenyl) bonds in various alkenes and 1,3-dienes could be cleaved via a hydrometalation and followed by β-carbon elimination pathway for Suzuki-Miyaura reactions. Furthermore, a series of novel organic fluorescent mols. with excellent photophys. properties were efficiently constructed with this protocol.

Angewandte Chemie, International Edition published new progress about Alkenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 13788-92-6 belongs to class pyrazoles-derivatives, and the molecular formula is C9H7BrN2, Synthetic Route of 13788-92-6.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Klug, Dana M.; Diaz-Gonzalez, Rosario; DeLano, Travis J.; Mavrogiannaki, Eftychia M.; Buskes, Melissa J.; Dalton, Raeann M.; Fisher, John K.; Schneider, Katherine M.; Hilborne, Vivian; Fritsche, Melanie G.; Simpson, Quillon J.; Tear, Westley F.; Devine, William G.; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Ruiz-Perez, Luis Miguel; Gamarro, Francisco; Gonzalez-Pacanowska, Dolores; Martinez-Martinez, Maria Santos; Manzano-Chinchon, Pilar; Navarro, Miguel; Pollastri, Michael P.; Ferrins, Lori published the artcile< Structure-property studies of an imidazoquinoline chemotype with antitrypanosomal activity>, Application In Synthesis of 1046832-21-6, the main research area is imidazoquinoline chemotype antitrypanosomal activity structure activity relationship.

Human African trypanosomiasis is a neglected tropical disease (NTD) that is fatal if left untreated. Although approx. 13 million people live in moderate- to high-risk areas for infection, current treatments are plagued by problems with safety, efficacy, and emerging resistance. In an effort to fill the drug development pipeline for HAT, we have expanded previous work exploring the chemotype represented by the compound NEU-1090, with a particular focus on improvement of absorption, distribution, metabolism and elimination (ADME) properties. These efforts resulted in several compounds with substantially improved aqueous solubility, although these modifications typically resulted in a loss of trypanosomal activity. We herein report the results of our investigation into the antiparasitic activity, toxicity, and ADME properties of this class of compounds in the interest of informing the NTD drug discovery community and avoiding duplication of effort.

RSC Medicinal Chemistry published new progress about Blood. 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Application In Synthesis of 1046832-21-6.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Zhou, You; Wang, Li-Sheng; Lei, Shuang-Gui; Gao, Yun-Xiang; Ma, Jin-Tian; Yu, Zhi-Cheng; Wu, Yan-Dong; Wu, An-Xin published the artcile< I2-Promoted site-selective C-C bond cleavage of aryl methyl ketones as C1 synthons for constructing 5-acyl-1H-pyrazolo[3,4-b]pyridines>, Recommanded Product: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, the main research area is aryl methyl ketone aminopyrazole enaminone iodine cleavage cyclization; pyrazolopyridine regioselective preparation.

A novel iodine promoted [1 + 3 + 2] cleavage cyclization reaction for the synthesis of 1H-pyrazolo[3,4-b]pyridines from aryl Me ketones, 5-aminopyrazoles and enaminones was established. This transition metal-free catalysis method has simple reaction conditions and good substrate compatibility, and was demonstrated in the transformation of alkyl and natural mol.-derived enaminones. Mechanistic studies showed that two cyclization pathways affording different key intermediates were involved, but affording the same target product after site-selective cleavage of the unstrained C-C bond of the acyl group.

Organic Chemistry Frontiers published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Recommanded Product: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Jain, Rama; Mathur, Michelle; Lan, Jiong; Costales, Abran; Atallah, Gordana; Ramurthy, Savithri; Subramanian, Sharadha; Setti, Lina; Feucht, Paul; Warne, Bob; Doyle, Laura; Basham, Stephen; Jefferson, Anne B.; Lindvall, Mika; Appleton, Brent A.; Shafer, Cynthia M. published the artcile< Discovery of Potent and Selective RSK Inhibitors as Biological Probes>, Category: pyrazoles-derivatives, the main research area is difluorophenol pyridine RSK inhibitor preparation antitumor.

While the p90 ribosomal S6 kinase (RSK) family has been implicated in multiple tumor cell functions, the full understanding of this kinase family has been restricted by the lack of highly selective inhibitors. A bis-phenol pyrazole was identified from high-throughput screening as an inhibitor of the N-terminal kinase of RSK2. Structure-based drug design using crystallog., conformational anal., and scaffold morphing resulted in highly optimized difluorophenol pyridine inhibitors of the RSK kinase family as demonstrated cellularly by the inhibition of YB1 phosphorylation. These compounds provide for the first time in vitro tools with an improved selectivity and potency profile to examine the importance of RSK signaling in cancer cells and to fully evaluate RSK as a therapeutic target.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 13808-65-6 belongs to class pyrazoles-derivatives, and the molecular formula is C9H7BrN2, Category: pyrazoles-derivatives.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Zhang, Juan; Li, Xianfeng; Wei, Haimei; Li, Yangfeng; Zhang, Gong; Li, Yizhou published the artcile< Sequential DNA-Encoded Building Block Fusion for the Construction of Polysubstituted Pyrazoline Core Libraries>, Application of C7H11N3, the main research area is aryl amine DNA encoded aldehyde cyclization; encoded DNA tetrazole preparation alkene cycloaddition; DNA encoded pyrazoline preparation.

Herein, a sequential DNA-encoded synthesis strategy for polysubstituted pyrazoline heterocycles, which fuses a broad panel of aldehydes, aryl amines, and alkenes as building blocks was reported. Furthermore, mock library synthesis and selection demonstrated the ability of the method to produce DNA-encoded focused libraries with highly functionalized pyrazoline cores.

Organic Letters published new progress about 1,3-Dipolar cycloaddition reaction. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Application of C7H11N3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Schantl, J. G. published the artcile< Product class 19: azomethine imines>, Reference of 17827-61-1, the main research area is review azomethine imine preparation organic synthesis.

A review. Methods for preparing azomethine imines and their application to organic synthesis.

Science of Synthesis published new progress about Imines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (azomethine). 17827-61-1 belongs to class pyrazoles-derivatives, and the molecular formula is C6H8N2O2, Reference of 17827-61-1.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Klug, Dana M.; Diaz-Gonzalez, Rosario; DeLano, Travis J.; Mavrogiannaki, Eftychia M.; Buskes, Melissa J.; Dalton, Raeann M.; Fisher, John K.; Schneider, Katherine M.; Hilborne, Vivian; Fritsche, Melanie G.; Simpson, Quillon J.; Tear, Westley F.; Devine, William G.; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Ruiz-Perez, Luis Miguel; Gamarro, Francisco; Gonzalez-Pacanowska, Dolores; Martinez-Martinez, Maria Santos; Manzano-Chinchon, Pilar; Navarro, Miguel; Pollastri, Michael P.; Ferrins, Lori published the artcile< Structure-property studies of an imidazoquinoline chemotype with antitrypanosomal activity>, Application of C10H17BN2O2, the main research area is imidazoquinoline chemotype antitrypanosomal activity structure activity relationship.

Human African trypanosomiasis is a neglected tropical disease (NTD) that is fatal if left untreated. Although approx. 13 million people live in moderate- to high-risk areas for infection, current treatments are plagued by problems with safety, efficacy, and emerging resistance. In an effort to fill the drug development pipeline for HAT, we have expanded previous work exploring the chemotype represented by the compound NEU-1090, with a particular focus on improvement of absorption, distribution, metabolism and elimination (ADME) properties. These efforts resulted in several compounds with substantially improved aqueous solubility, although these modifications typically resulted in a loss of trypanosomal activity. We herein report the results of our investigation into the antiparasitic activity, toxicity, and ADME properties of this class of compounds in the interest of informing the NTD drug discovery community and avoiding duplication of effort.

RSC Medicinal Chemistry published new progress about Blood. 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Application of C10H17BN2O2.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Wang, Dinghai; Wu, Lianqian; Wang, Fei; Wan, Xiaolong; Chen, Pinhong; Lin, Zhenyang; Liu, Guosheng published the artcile< Asymmetric Copper-Catalyzed Intermolecular Aminoarylation of Styrenes: Efficient Access to Optical 2,2-Diarylethylamines>, Synthetic Route of 936250-20-3, the main research area is asym copper catalyzed intermol aminoarylation styrene alkylsulfonamide; diarylethylamine preparation.

We have developed a copper-catalyzed enantioselective intermol. aminoarylation of alkenes using a novel N-fluoro-N-alkylsulfonamide as the amine reagent, which could react with the Cu(I) catalyst to release a related amino radical. After addition to styrene, the generated benzylic radical could couple with a chiral L*CuIIAr complex to achieve enantioselective arylation. Various optical 2,2-diarylethylamines were efficiently synthesized from simple styrenes with high enantioselectivity, and these products can serve as valuable synthons toward bioactive mols.’ synthesis.

Journal of the American Chemical Society published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 936250-20-3 belongs to class pyrazoles-derivatives, and the molecular formula is C10H17BN2O2, Synthetic Route of 936250-20-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Nemec, Vaclav; Hylsova, Michaela; Maier, Lukas; Flegel, Jana; Sievers, Sonja; Ziegler, Slava; Schroeder, Martin; Berger, Benedict-Tilman; Chaikuad, Apirat; Valcikova, Barbora; Uldrijan, Stjepan; Drapela, Stanislav; Soucek, Karel; Waldmann, Herbert; Knapp, Stefan; Paruch, Kamil published the artcile< Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway>, Recommanded Product: 1-Phenyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, the main research area is synthesis furopyridine; furopyridine cdc like kinase inhibitor Hedgehog pathway modulator; biological activity; chemical probes; heterocycles; inhibitors; kinases.

Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic sequences based on chemoselective metal-mediated couplings, including assembly of the furo[3,2-b]pyridine scaffold by copper-mediated oxidative cyclization. Optimization of the subseries containing 3,5-disubstituted furo[3,2-b]pyridines, e.g. I, afforded potent, cell-active, and highly selective inhibitors of CLKs. Profiling of the kinase-inactive subset of 3,5,7-trisubstituted furo[3,2-b]pyridines, e.g. II, revealed sub-micromolar modulators of the Hedgehog pathway.

Angewandte Chemie, International Edition published new progress about Antitumor agents. 1002334-12-4 belongs to class pyrazoles-derivatives, and the molecular formula is C15H19BN2O2, Recommanded Product: 1-Phenyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Witiak, Donald T.; Lu, Matthias C. published the artcile< Product ratio analysis of the reaction of methyl cis- and trans-β-(acetylthio)acrylates with diazomethane>, Recommanded Product: Methyl 1-Methylpyrazole-3-carboxylate, the main research area is pyrazoles from acetylthioacrylates diazomethanation; acetylthioacrylates diazomethanation pyrazoles from; diazomethanation acetylthioacrylates pyrazoles from.

The relative yield of Me cis-β-(methylmercapto)acrylate 1-methyl-5-carbomethoxypyrazole 3-carbomethoxypyrazole and 1-methyl-3-carbomethoxypyrazole when Me cis- or trans-β-(acetylthio)acrylate undergoes reaction with excess CH2N2 in ether, was determined by means of gas-liquid partition chromatog. The analysis shows product formation to be dependent upon the stereochemistry of the starting Me β-(acetylthio)acrylate. Competing reaction pathways are proposed to account for the different yields of products. 25 references.

Journal of Organic Chemistry published new progress about 17827-61-1. 17827-61-1 belongs to class pyrazoles-derivatives, and the molecular formula is C6H8N2O2, Recommanded Product: Methyl 1-Methylpyrazole-3-carboxylate.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics