Tag: M.W=150-200

Zhang, Cheng; Hong, Kemiao; Dong, Shanliang; Pei, Chao; Zhang, Xiaolu; He, Ciwang; Hu, Wenhao; Xu, Xinfang published the artcile< Gold(I)-Catalyzed Aromatization: Expeditious Synthesis of Polyfunctionalized Naphthalenes>, Product Details of C10H9NO2, the main research area is polyfunctionalized naphthalene preparation; alkynyl diazoacetate endo dig carbocyclization gold catalyst; Catalysis; Organic Reaction; Organic Synthesis.

A gold-catalyzed 6-endo-dig carbocyclization of alkyne with the pendent diazo group is reported. It provides an expeditious approach for the synthesis of multi-functionalized naphthalene derivatives under mild conditions. Mechanistic studies suggest that a vinyl gold carbene is generated as the key intermediate in this cascade transformation that smoothly delivers naphthalene products through an unprecedented stepwise aromatization or an intermol. aromatic substitution process. The unique endocyclic vinyl species is inaccessible with other precursors; thus, novel carbene cascade transformations could be envisioned with the current catalytic model. Functional groups, such as alkenyl, hydroxyl, amino, and carboxyl groups, remain untouched under these conditions. In addition, the utility of these generated 2-carboxyl naphthalenes is illustrated by the synthesis of chiral 1,2′-binaphthalene ligands and π-conjugated polycyclic hydrocarbons (CPHs).

iScience published new progress about Alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, Product Details of C10H9NO2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Xie, Xiu-Ying; Jiang, Wei-Tao; Xiao, Bin published the artcile< Alkyl Carbagermatrane Enabled Synthesis of Seven-Membered Carbocycle-Fused Aromatics through Catellani Strategy>, Reference of 93247-78-0, the main research area is bromoalkyl carbagermatrane preparation iodoarene palladium phosphine regioselective Catellani cyclization; carbocycle fused arene preparation.

Synthesis of seven-membered carbocycle-fused aromatics was realized by Catellani reaction using terminally brominated alkyl carbagermatranes through intermol. cyclization manner. Various functional groups were well tolerated and this transformation was also expanded to the synthesis of carbocycles of other size. The utility of the above method was demonstrated by modification of natural product derivatives and synthesis of bioactive mols.

Synthesis published new progress about Aliphatic esters Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, Reference of 93247-78-0.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Schlegel, Marcel; Schneider, Christoph published the artcile< Iron(III)-Catalyzed (4 + 2)-Cycloannulation of 2-Hydroxy Ketoxime Ethers with Indol-2-ylamides: Synthesis of Indole-Fused 2-Piperidinones>, Quality Control of 399-76-8, the main research area is indole fused piperidinone diastereoselective preparation; hydroxy ketoxime ether indolecarboxamide cycloaddition iron catalyst.

A highly regio- and diastereoselective (4 + 2)-cycloannulation process of indanone-derived 2-hydroxy ketoxime ethers with 1,4-bisnucleophilic indol-2-ylamides has been developed. In the presence of 5 mol % FeCl3, densely functionalized 2-piperidinones containing two new σ-bonds and two vicinal quaternary stereogenic centers were formed under mild reaction conditions in a one-pot operation. Moreover, most of the products directly precipitated out of the solution and were isolated by simple filtration without purification by column chromatog.

Journal of Organic Chemistry published new progress about [4+2] Cycloaddition reaction. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Quality Control of 399-76-8.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Allred, Tyler K.; Shaghafi, Michael B.; Chen, Pan-Pan; Tran, Quan; Houk, K. N.; Overman, Larry E. published the artcile< Constructing Saturated Guanidinium Heterocycles by Cycloaddition of N-Amidinyliminium Ions with Indoles>, COA of Formula: C10H9NO, the main research area is guanidinium heterocycle preparation indole amidinyliminium regioselective stereoselective cycloaddition.

We report that structurally complex guanidinium heterocycles can be prepared in one step by regio- and stereoselective [4 + 2]-cycloadditions of N-amidinyliminium ions with indoles or benzothiophene. In contrast to reactions of these heterodienes with alkenes, d. functional theory (DFT) calculations show that these cycloadditions take place in a concerted asynchronous fashion. The [4 + 2]-cycloaddition of N-amidinyliminium ions (1,3-diaza-1,3-dienes) with indoles and benzothiophene are distinctive, as related [4 + 2]-cycloadditions of N-acyliminium ions (1-oxa-3-aza-1,3-dienes) are apparently unknown.

Organic Letters published new progress about [4+2] Cycloaddition reaction. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, COA of Formula: C10H9NO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Sako, Kumiko; Aoyama, Hiroshi; Sato, Shinichi; Hashimoto, Yuichi; Baba, Masanori published the artcile< γ-Carboline derivatives with anti-bovine viral diarrhea virus (BVDV) activity>, COA of Formula: C10H9NO, the main research area is bovine viral diarrhea virus carboline derivative preparation SAR.

Based on anti-viral screening of our heteroaromatics derived from thalidomide, the γ-carboline skeleton has been identified as a superior scaffold structure for compounds with potent anti-bovine viral diarrhea virus (BVDV) activity. BVDV is thought to be a good model for human hepatitis C virus. Structural development studies led to a potent anti-viral agent, SK5M (5-methyl-γ-carboline), with the EC50 of 0.26 μM.

Bioorganic & Medicinal Chemistry published new progress about Antiviral agents. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, COA of Formula: C10H9NO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Yoo, Woo-Jin; Nguyen, Thanh V. Q.; Capdevila, Montse Guiteras; Kobayashi, Shu published the artcile< Lithium tert-butoxide-mediated carboxylation reactions of unprotected indoles and pyrroles with carbon dioxide>, SDS of cas: 23077-43-2, the main research area is indole carbon dioxide lithium butoxide Friedel Crafts type carboxylation; indolecarboxylic acid preparation; pyrrole carbon dioxide lithium butoxide Friedel Crafts type carboxylation; pyrrolecarboxylic acid preparation.

Unprotected indoles and pyrroles were found to underwent base-mediated carboxylation reactions under ambient pressure of carbon dioxide. It was found that this transition metal-free carboxylation reaction proceeded smoothly with the use of a large excess of LiOtBu.

Heterocycles published new progress about Aromatic carboxylic acids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, SDS of cas: 23077-43-2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Li, Honghe; Yan, Xiaoqiang; Zhang, Jitan; Guo, Weicong; Jiang, Jijun; Wang, Jun published the artcile< Enantioselective Synthesis of C-N Axially Chiral N-Aryloxindoles by Asymmetric Rhodium-Catalyzed Dual C-H Activation>, Product Details of C8H6ClNO, the main research area is arylnaphthyl oxindole atropisomer enantioselective preparation; rhodium catalyst enantioselective activation cycloaddition aryl alkyne aryloxindole; C−H activation; alkynes; axial chirality; heterocycles; rhodium.

In the presence of a diindolocyclononane-fused cyclopentadiene rhodium complex and AgNTf2, N-aryloxindoles such as I underwent enantioselective Satoh-Miura-type cycloaddition reactions with diaryl alkynes such as diphenylacetylene to yield atropisomeric tetraarylnaphthyl oxindoles such as II in up to 99% yield and in 8-99% ee (all but one product in >60% ee).

Angewandte Chemie, International Edition published new progress about Atropisomers. 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Product Details of C8H6ClNO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Li, Ruo-Pu; Wang, Zheng-Lin; Zhang, Yun-Hao; Tan, Zhi-Yu; Xu, Da-Zhen published the artcile< Iodine-Catalyzed Oxidative Coupling of Indolin-2-ones with Indoles: Synthesis of 3,3-Disubstituted Oxindole Compounds>, Application of C8H6ClNO, the main research area is disubstituted oxindole preparation; indolinone indole oxidative coupling iodine catalyst.

Here, an iodine-catalyzed oxidative coupling of indolinones with indoles for the construction of compounds with all-carbon quaternary centers such as 1H,1”H-[3,3′:3′,3”-terindol]-2′(1’H)-ones I [R1 = H, Me, Bn, etc.; R2 = H, 5-Br, 5-F, etc.; R3 = H, Me, R4 = H, 2-Me, 5-OMe, etc.] was described. The method performed under metal-free and peroxide-free conditions, providing 3,3-disubstituted oxindoles via two C-C bond formations from secondary C(sp3)-Hs in a straightforward manner.

ChemistrySelect published new progress about C-C bond formation. 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Application of C8H6ClNO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wu, Ke-Xin; Xu, Yi-Ze; Cheng, Liang; Wu, Run-Shi; Liu, Peng-Ze; Xu, Da-Zhen published the artcile< Iron-catalyzed oxidative bis-arylation of indolin-2-ones for direct construction of quaternary carbons>, Computed Properties of 20870-77-3, the main research area is oxindole bis indolyl preparation chemoselective green chem; indolinone indole oxidative bis arylation iron catalyst.

A direct construction of all-carbon quaternary centers from secondary C(sp3)-H substrates through a dehydrogenative cross-coupling reaction was described. Using FeCl2·4H2O as the catalyst and employing air (mol. oxygen) as the terminal oxidant, the cross-coupling of indolin-2-ones I (R1 = H, Me, Ph, Bn; R2 = H, 6-Cl, 5-F, etc.) with indoles such as 5-fluoroindole, N-methylindole, 3-methylindole, etc. proceeded smoothly under mild, ligand-free and base-free conditions, providing 3,3-disubstituted oxindoles bearing all-carbon quaternary centers II (R3 = 5-fluoroindol-3-yl, N-methylindol-3-yl, 3-methylindol-2-yl, etc.) with excellent chemoselectivities.

Green Chemistry published new progress about Arylation (chemoselective). 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Computed Properties of 20870-77-3.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Becker, Daniel P.; Flynn, Daniel L.; Moormann, Alan E.; Nosal, Roger; Villamil, Clara I.; Loeffler, Richard; Gullikson, Gary W.; Moummi, Chafiq; Yang, Dai-C. published the artcile< Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists>, Name: 5-Fluoro-1H-indole-3-carboxylic acid, the main research area is pyrrolizidine arylamide preparation 5HT4 antagonist; arylester pyrrolizidine preparation 5HT4 agonist.

A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT4 and 5-HT3 receptor binding, 5-HT4 receptor agonism in the rat tunica muscularis mucosae assay (TMM), and for 5-HT3 receptor-mediated functional antagonism in the Bezold-Jarisch reflex assay. Several pyrrolizidine derivatives were identified with high affinity for the 5-HT4 receptor, including benzamide I (SC-53116), a potent and selective 5-HT4 partial agonist that exhibits efficacy in promoting antral contractions and activity in promoting gastric emptying in canine models. Also discovered were 5-HT4 receptor antagonists, including imidazopyridine amide II (SC-53606), which was a potent and selective 5-HT4 receptor antagonist with a pA2 value of 8.13 in the rat TMM assay. N-Me indole ester III was identified as a potent 5-HT4 antagonist with a pA2 value of 8.93. High selectivity was observed for these pyrrolizidine derivatives vs. other monoamine receptors, including 5-HT1, 5-HT2, D1, D2, α1, α2, and β receptors.

Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Name: 5-Fluoro-1H-indole-3-carboxylic acid.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles