Tag: M.W=150-200

Hu, Yijie; Ye, Liufeiyang; Chen, Jie; Zhang, Hui; Deng, Hongmei; Lin, Jin-Hong; Cao, Weiguo published the artcile< An Efficient Construction of CF3-Substituted Spirooxindole-Fused Benzo[a]quinolizidines by a Three-Component Cyclization>, Recommanded Product: 5-Methoxyisoquinoline, the main research area is isoquinoline perfluoroalkylpropiolate oxoindolinylidene propanedinitrile three component cyclization; perfluoroalkyl dicyano spirooxindoline benzoquinolizidine carboxylate preparation.

A convenient three-component cyclization was described for the efficient construction of CF3-substituted spirooxindole-fused benzo[a]quinolizidines by using CF3-propiolate as a building block. This attractive protocol may find great synthetic utility since CF3-containing complex structures were installed by a one-step cyclization under mild conditions.

European Journal of Organic Chemistry published new progress about Alkynes, fluoro Role: RCT (Reactant), RACT (Reactant or Reagent). 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Recommanded Product: 5-Methoxyisoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Berthel, Steven J.; Marks, Ian M.; Yin, Xuefeng; Mischke, Steven G.; Orzechowski, Lucja; Pezzoni, Gabriella; Sala, Franca; Vassilev, Lyubomir T. published the artcile< Identification of phenyl-pyridine-2-carboxylic acid derivatives as novel cell cycle inhibitors with increased selectivity for cancer cells>, Application In Synthesis of 721401-43-0, the main research area is phenylpyridine carboxylate derivative preparation structure activity antitumor cell cycle; Ro414439 cell cycle antitumor breast cancer mitosis structure activity.

Ro 41-4439, a phenyl-pyridine-2-carboxylic acid derivative, was identified by a cell-based screening approach that exploits the differences between normal and cancer cells in their sensitivity to cytotoxic agents. This compound showed low micromolar antiproliferative activity and cytotoxicity against a broad panel of human cancer cell lines in vitro, and over 10-fold selectivity to cancer cells when tested in parallel with a panel of proliferating normal human cells. Cytotoxicity of Ro 41-4439 is due to arrest of cell cycle progression in mitosis followed by induction of apoptosis. Four-week treatment of nude mice bearing established mammary tumor xenografts (MDA-MB-435) with well-tolerated doses of the compound showed 73% inhibition of tumor growth. Limited exploration of structure-activity relationships involving side chain length, and aryl and pyridine rings allowed for the identification of more potent analogs.

Anti-Cancer Drugs published new progress about Antitumor agents. 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, Application In Synthesis of 721401-43-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Favalli, Nicholas; Bassi, Gabriele; Bianchi, Davide; Scheuermann, Jorg; Neri, Dario published the artcile< Large screening of DNA-compatible reaction conditions for Suzuki and Sonogashira cross-coupling reactions and for reverse amide bond formation>, COA of Formula: C9H8BNO2, the main research area is alkyne pinacol borane boronic acid DNA synthesis carboxylic acid; Suzuki Sonogashira cross coupling reverse amide formation DNA compatible; DNA-compatible reactions; DNA-encoded libraries; Reverse amide bond formation; Sonogashira cross-coupling; Suzuki cross-coupling.

Progress in DNA-encoded chem. library synthesis and screening crucially relies on the availability of DNA-compatible reactions, which proceed with high yields and excellent purity for a large number of possible building blocks. In the past, exptl. conditions have been presented for the execution of Suzuki and Sonogashira cross-coupling reactions on-DNA. In this article, our aim was to optimize Suzuki and Sonogashira reactions, comparing our results to previously published procedures. We have tested the performance of improved conditions using 606 building blocks (including boronic acids, pinacol boranes and terminal alkynes), achieving >70% conversion for 84% of the tested mols. Moreover, we describe efficient exptl. conditions for the on-DNA synthesis of amide bonds, starting from DNA derivatives carrying a carboxylic acid moiety and 300 primary, secondary and aromatic amines, as amide bonds are frequently found in DNA-encoded chem. libraries thanks to their excellent DNA compatibility.

Bioorganic & Medicinal Chemistry published new progress about Boronic acids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, COA of Formula: C9H8BNO2.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Tao; Liang, Kangjiang; Zhang, Yang; Hu, Dongyan; Ma, Zhixian; Xia, Chengfeng published the artcile< Three-Component Minisci Reaction with 1,3-Dicarbonyl Compounds Induced by Visible Light>, Name: 5-Methoxyisoquinoline, the main research area is quinoline preparation visible light Minisci dicarbonyl vinyl ether heterocycle; isoquinoline preparation visible light Minisci dicarbonyl vinyl ether heterocycle.

A three-component Minisci reaction coupling of 1,3-dicarbonyl compounds with vinyl ethers and quinolines or isoquinolines under visible light is developed. The 1,3-dicarbonyl compound undergoes single-electron oxidation to afford an electrophilic 1,3-dicarbonyl radical under visible light irradiation Due to the polarity of the free radical, the electrophilic radical adds to the electron-rich olefin to afford the nucleophilic radical. It coupled with the heteroarene to afford the three-component coupling products.

Organic Letters published new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Name: 5-Methoxyisoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Dong, Jianyang; Yue, Fuyang; Liu, Jianhua; Song, Hongjian; Liu, Yuxiu; Wang, Qingmin published the artcile< Visible-light-mediated three-component Minisci reaction for heteroarylethyl alcohols synthesis>, Application In Synthesis of 90806-58-9, the main research area is heteroarylethyl alc green diastereoselective preparation; heteroaryl alkene three component Minisci visible light iridium catalyst.

Herein, a mild, modular, practical Minisci reaction for catalytic synthesis of heteroarylethyl alcs. such as ArCH(R1)CHR2OH [Ar = quinol-2-yl, isoquinolin-1-yl, 2-benzothiazolyl, etc.; R1R2 = CH2(CH2)2CH2, CH2CH2CH2; R1 = On-Bu, Me; R2 = H, Me] via sequential addition of H2O and N-heteroarenes across olefinic double bonds was reported. This scalable protocol was used for direct hydroxy-heteroarylation of olefins with a wide range of N-heteroarenes and could be expected to permit rapid conversion of abundant feedstock materials into medically relevant mols.

Green Chemistry published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation) (heteroarylethyl). 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Application In Synthesis of 90806-58-9.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Su, Yong-Liang; Liu, Geng-Xin; De Angelis, Luca; He, Ru; Al-Sayyed, Ammar; Schanze, Kirk S.; Hu, Wen-Hao; Qiu, Huang; Doyle, Michael P. published the artcile< Radical Cascade Multicomponent Minisci Reactions with Diazo Compounds>, Quality Control of 90806-58-9, the main research area is heteroarene preparation regioselective photochem; aromatic heterocycle alkene diazo compound tandem multicomponent Minisci iridium.

Based on the strategy of polarity reversal in the generation of free radicals derived from diazo compounds, R1C(=N2)R2[R1 = ethoxycarbonyl, (benzyloxy)carbonyl, N,N-diethylcarbamoyl, etc.; R2 = H, C(O)OMe] photocatalyzed multicomponent reactions (MCRs) of nitrogen aromatic heterocycles, e.g., 4-methylquinoline, alkenes R3CH=CH2 [R3 = methoxymethyl, cyclohexyl, 4-[(furan-2-yl)carbonyloxy]butyl, etc.], and diazo compounds form functionalized derivatives e.g., Et 4-(4-methylquinolin-2-yl)-6-phenylhexanoate in good to high yields and exacting regioselectivities. The carbon radicals generated from the acceptor diazo compounds are electrophilic, and their selective additions with alkenes provide nucleophilic radicals, which enable the further rapid assembly with various heteroarenes. A delicate balance has been achieved between the activation of heteroarenes through protonation and the decomposition of diazo compounds by the same acid. This multicomponent Minisci reaction shows high functional group tolerance, especially in the incorporation of biol. active mols. Detailed mechanistic studies that include photophys. measurements elaborate this radical cascade reaction. Furthermore, this transformation provides new opportunities for versatile reactions of diazo compounds in radical cascade multicomponent coupling reactions.

ACS Catalysis published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Quality Control of 90806-58-9.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

He, Zhen-Hong; Wei, Yuan-Yuan; Li, Na; Sun, Yong-Chang; Yang, Shao-Yan; Wang, Kuan; Wang, Weitao; Ma, Xiaoxue; Liu, Zhao-Tie published the artcile< N-formylation of isoquinoline derivatives with CO2 and H2 over a heterogeneous Ru/ZIF-8 catalyst>, Recommanded Product: 5-Methoxyisoquinoline, the main research area is isoquinoline derivative formylation heterogeneous calayst property.

Chem. utilization of CO2 is one of the fundamental strategies to synthesize value-added chems. and reduce the CO2 emission. N-formyl-1,2,3,4-tetrahydroisoquinoline derivatives (FTHIQs) are important chems. for the synthesis of medical intermediates and alkaloids. N-formylation of isoquinoline derivatives (IQs) with CO2 is an ideal protocol to synthesize the FTHIQs and utilize the CO2 source. In the present work, we prepared a heterogeneous Ru/ZIF-8 catalyst with a Ru loading of 2 wt% by a simple impregnation method and assessed its performances in the N-formylation of IQs and CO2 with H2. The Ru/ZIF-8 catalyst offered high IQ conversion of 98% and FTHIQ selectivity of 93% in the reaction under relatively mild conditions (150°C, 2 MPa CO2, and 6 MPa H2). The catalyst possessed good universality and reusability, showing a potential in wide application of N-formylation of highly unsaturated nitrogen-containing isoquinolines.

Journal of Experimental Nanoscience published new progress about Catalyst supports. 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Recommanded Product: 5-Methoxyisoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Shasha; Pissarnitski, Dmitri; Nowak, Timothy; Wleklinski, Michael; Krska, Shane W. published the artcile< Merging Late-Stage Diversification with Solid-Phase Peptide Synthesis Enabled by High-Throughput On-Resin Reaction Screening>, HPLC of Formula: 721401-43-0, the main research area is solid phase peptide synthesis high throughput experimentation; Suzuki Miyaura coupling peptide boronic acid library.

An integrated workflow is described that combines micromole-scale high-throughput experimentation (HTE) reaction screening and solid-phase peptide synthesis (SPPS) to enable rapid synthetic method development for on-resin peptide diversification. Using this new approach, we have identified several sets of robust Suzuki-Miyaura coupling conditions with complementary scope that collectively display broad coverage with respect to both resin-bound peptide substrates containing aryl halide side chains and (hetero)arylboronic acid coupling partners. We have also demonstrated the utility of this integrated SPPS/chem. diversification method by synthesizing a multidimensional library of diverse peptides in high yields.

ACS Catalysis published new progress about Amino acids Role: CMB (Combinatorial Study), RCT (Reactant), RACT (Reactant or Reagent). 721401-43-0 belongs to class isoquinoline, and the molecular formula is C9H8BNO2, HPLC of Formula: 721401-43-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Zhou, Wei; Liu, Hao; Guo, Yongyi; Gu, Yiting; Han, Jing; Chen, Jie; Deng, Hongmei; Shao, Min; Zhang, Hui; Cao, Weiguo published the artcile< Base-promoted [3+2] cycloaddition/aromatization cascade reaction under air: An approach to access perfluoroalkylated pyrrolo[2,1-a]isoquinolines>, Synthetic Route of 90806-58-9, the main research area is isoquinoline bromomethyl aryl ketone perfluoroalkynoate dipolar cycloaddition aromatization cascade; pyrroloisoquinoline perfluoroalkylated preparation.

A facile [3 + 2] cycloaddition / aromatization cascade reaction with broad substrate scopes in up to 94% isolated yield was disclosed herein. This tandem approach was accomplished by employing isoquinolines and bromoacetyl derivatives with Me perfluoroalk-2-ynoates as readily available starting materials. In the presence of base, this method provides an efficient access to synthesize perfluoroalkylated pyrrolo[2,1-a]isoquinolines with ambient air as a terminal oxidant at room temperature in one-pot.

Journal of Fluorine Chemistry published new progress about 1,3-Dipolar cycloaddition reaction. 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Synthetic Route of 90806-58-9.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Huang, Cheng; Wang, Jing-Hao; Qiao, Jia; Fan, Xiu-Wei; Chen, Bin; Tung, Chen-Ho; Wu, Li-Zhu published the artcile< Direct Arylation of Unactivated Alkanes with Heteroarenes by Visible-Light Catalysis>, Synthetic Route of 90806-58-9, the main research area is alkane heteroarene arylation iridium visible light; alkylheteroarene preparation; iridium visible light arylation catalyst.

The functionalization of aliphatic C-H bonds is both a major challenge and a desirable goal in organic synthesis. Here, a successful arylation of unactivated alkanes with heteroarenes by using iridium polypyridyl complexes as the photocatalyst and persulfate as the HAT catalyst precursor under visible-light irradiation, is described. This reaction features good functional group tolerance and broad scope with regard to both alkane and heteroarene substrates (37 examples), which allows direct access to alkyl-substituted N-heteroarenes, a key structural motif in natural products and bioactive mols.

Journal of Organic Chemistry published new progress about Alkanes Role: RCT (Reactant), RACT (Reactant or Reagent). 90806-58-9 belongs to class isoquinoline, and the molecular formula is C10H9NO, Synthetic Route of 90806-58-9.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem