Tag: M.W=200-250

Kumar, G. Santosh published the artcileCatalyst-free synthesis of 3-hydroxy-3-(alkyl/aryl)indolin-2-ones by addition of organoaluminum reagents to isatins, SDS of cas: 1677-47-0, the main research area is isatin organoaluminum reagent addition; alkyl hydroxyindolinone preparation; phenyl hydroxyindolinone preparation.

An efficient synthesis of 3-hydroxy-3-(alkyl/aryl)indol-2-one derivatives I (R = H, Me, Bn; R1 = H, Cl, Br; R2 = H, Cl, Br, I, F, OCF3, NO2; R3 = H, Cl, Br) has been described by the reactions of isatin with organoaluminum reagents. The reaction is very rapid and yields are high. The protocol is applicable for substituted isatins as well as a variety of organoaluminums.

Tetrahedron Letters published new progress about Addition reaction. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, SDS of cas: 1677-47-0.

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

Li, Xiang published the artcileAerobic Transition-Metal-Free Visible-Light Photoredox Indole C-3 Formylation Reaction, Quality Control of 13523-93-8, the main research area is indole TMEDA oxygen Rose Bengal visible light photoredox formylation; formyl indole regioselective preparation.

An aerobic visible-light-promoted indole C-3 formylation reaction catalyzed by Rose Bengal has been developed. This transition-metal-free process employs mol. oxygen as the terminal oxidant and uses TMEDA as the one-carbon source through C-N bond cleavage. The reaction is compatible with a variety of functional groups.

ACS Catalysis published new progress about C-N bond cleavage. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Quality Control of 13523-93-8.

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

Sirisoma, Nilantha published the artcileDiscovery of substituted N’-(2-oxoindolin-3-ylidene)benzohydrazides as new apoptosis inducers using a cell- and caspase-based HTS assay, Computed Properties of 1677-47-0, the main research area is antitumor oxoindolinylidenebenzohydrazide preparation apoptosis neoplasm.

The discovery of a series of substituted N’-(2-oxoindolin-3-ylidene)benzohydrazides as inducers of apoptosis using a proprietary cell- and caspase-based ASAP HTS assay is reported. Through SAR studies, N’-(4-bromo-5-methyl-2-oxoindolin-3-ylidene)-3,4,5-trimethoxybenzohydrazide (3g) was identified as a potent apoptosis inducer with an EC50 value of 0.24 μM in human colorectal carcinoma HCT116 cells, more than a 40-fold increase in potency from the initial screening hit N’-(5-bromo-2-oxoindolin-3-ylidene)-3,4,5-trimethoxybenzohydrazide (2a). Compound 3g also was found to be highly active in a growth inhibition assay with a GI50 value of 0.056 μM in HCT116 cells. A group of potentially more aqueous soluble analogs were prepared and found to be highly active. Among them, compound 4e incorporating a Me piperazine moiety was found to have EC50 values of 0.17, 0.088 and 0.14 μM in human colorectal carcinoma cells HCT116, hepatocellular carcinoma cancer SNU398 cells and human colon cancer RKO cells, resp. Compounds 3g and 4e were found to function as inhibitors of tubulin polymerization

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, Computed Properties of 1677-47-0.

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

Liang, Taoyuan published the artcileStraightforward access to novel indolo[2,3-b]indoles via aerobic copper-catalyzed [3+2] annulation of diarylamines and indoles, HPLC of Formula: 13523-93-8, the main research area is diarylamino indoloindole chemoselective preparation; diarylamine indole aerobic annulation copper catalyst.

An unprecedented aerobic copper-catalyzed [3+2] annulation reaction of diarylamines with indoles was reported, which allowed direct access to novel 2-diarylamino-indolo[2,3-b]indoles I [R = Ph, 4-MeC6H4, 4-ClC6H4, etc.; R1 = Me, Et, Bn, etc.; R2 = H, 4-Me, 6-F, etc.; Ar = Ph, 4-MeC6H4, 4-t-BuC6H4, etc.; Ar1 = Ph, 4-MeC6H4], a class of potential photoelec. device mols. The developed transformation proceeded with broad substrate scope, good functional group tolerance, high chemo-selectivity and no need for pre-preparation of specific agents, which offered a practical route for diverse and atom-economic synthesis of the desired products.

Chemical Communications (Cambridge, United Kingdom) published new progress about [3+2] Cycloaddition reaction. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, HPLC of Formula: 13523-93-8.

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

Ranasinghe, Nadeesha published the artcileExtending the versatility of the Hemetsberger-Knittel indole synthesis through microwave and flow chemistry, Safety of Methyl 6-nitro-1H-indole-2-carboxylate, the main research area is Hemetsberger Knittel indole synthesis microwave chem.

Microwave, flow and combination methodologies were applied to the synthesis of a number of substituted indoles. Based on the Hemetsberger-Knittel (HK) process, modifications allow formation of products rapidly and in high yield. Adapting the methodol. allows formation of 2-unsubstituted indoles and derivatives, and a route to analogs of the antitumor agent PLX-4032 is demonstrated. The utility of the HK substrates is further demonstrated through bioconjugation and subsequent ring closure and via Huisgen type [3+2] cycloaddition chem., allowing formation of peptide adducts which can be subsequently labeled with fluorine tags.

Bioorganic & Medicinal Chemistry Letters published new progress about [3+2] Cycloaddition reaction. 136818-66-1 belongs to class indole-building-block, name is Methyl 6-nitro-1H-indole-2-carboxylate, and the molecular formula is C10H8N2O4, Safety of Methyl 6-nitro-1H-indole-2-carboxylate.

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

Tong, Kun published the artcileVisible-Light-Induced Direct Oxidative C-H Amidation of Heteroarenes with Sulfonamides, Related Products of indole-building-block, the main research area is heterocyclic compound preparation regioselective photochem; heteroarene sulfonamide oxidative carbon hydrogen amidation iridium catalyst; C−H amidation; heterocycles; nitrogen-centered radicals; photochemistry; visible light.

A direct oxidative C-H amidation of heteroarenes, e.g., I, with sulfonamides RNHSO2R1 [R = CH3, C6H5, oxan-4-yl, etc.; R1 = CH3(CH2)4, C6H5, c-C3H5, pyridin-3-yl, etc.] via nitrogen-centered radicals has been described. Nitrogen-centered radicals are directly generated from oxidative cleavage of NH bonds under visible-light photoredox catalysis. Sulfonamides, which are easily accessed, used as tunable nitrogen sources. Bleach (aqueous NaClO solution), which is clean and economic, was used as the solely oxidant. A variety of heteroarenes, including indoles, pyrroles, and benzofurans, can undergo this amidation with high yields (up to 92%). These reactions are highly regioselective, and all the products, e.g., II, are isolated as single regioisomer.

Chemistry – A European Journal published new progress about Amidation (regioselective). 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Related Products of indole-building-block.

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

Maddela, Srinubabu published the artcileSynthesis of isatin-quinoline conjugates as possible biologically active agents, Recommanded Product: 4,5-Dichloroisatin, the main research area is isatin quinoline conjugate preparation antibacterial antifungal antiinflammatory; quinolinyl hydrazide isatin condensation.

A series of 12 new quinoline-3-carbohydrazide derivatives I (R = H, 5-F, 4-Cl, 7-Cl, etc.) were synthesized by the condensation of quinolinyl hydrazide with different isatins. The synthesized compounds were evaluated for in vitro antimicrobial and in vivo anti-inflammatory activity. Tested compounds exhibited moderate to good antibacterial and antifungal activity. Evaluation of the compounds revealed remarkable anti-inflammatory activity and were comparable with standard, indomethacin. Compounds I (R = 5-O2N, 5-F, 7-Cl, 4-Cl) inhibited paw edema in a carrageenan-induced rat hind paw edema model.

Toxicological & Environmental Chemistry published new progress about Anti-inflammatory agents. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, Recommanded Product: 4,5-Dichloroisatin.

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

Nishiyama, Takashi published the artcileConcise synthesis of carbazole-1,4-quinones and evaluation of their antiproliferative activity against HCT-116 and HL-60 cells, Application In Synthesis of 136818-66-1, the main research area is carbazolequinone preparation antiproliferative human; indole allyl alc tandem ring closing metathesis dehydrogenation; Antiproliferative activity; Carbazole-1,4-quinone; Koeniginequinone A; Koeniginequinone B.

A convenient synthesis of carbazole-1,4-quinone alkaloid koeniginequinones A and B using a tandem ring-closing metathesis with the dehydrogenation reaction sequence under an O2 atmosphere as an important step is reported. Using this method, carbazole-1,4-quinones substituted at the 5-, 6-, 7-, and/or 8-positions I (R1 = R2 = H, CH3; R3 = H, 6-OCH3, 5,6-(OCH3)2, 7-CH3, 6-NO2, etc.; R4 = H, MOM) have been synthesized. Moreover, 24 compounds, including koeniginequinones A and B, have been evaluated for their antiproliferative activity against HCT-116 and HL-60 cells, and the 6-nitro analog exhibited the most potent activity against both tumor cell types.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 136818-66-1 belongs to class indole-building-block, name is Methyl 6-nitro-1H-indole-2-carboxylate, and the molecular formula is C10H8N2O4, Application In Synthesis of 136818-66-1.

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

Koenig, Stefan G. published the artcileCopper-Catalyzed Synthesis of Indoles and Related Heterocycles in Renewable Solvents, Recommanded Product: Ethyl 6-cyano-1H-indole-2-carboxylate, the main research area is copper catalyst cross coupling acetamidoacetate bromobenzaldehyde renewable solvent; indolecarboxylate preparation green chem; fused heterocycle preparation green chem.

An efficient one-pot cascade to indoles and related fused heterocycles has been demonstrated in renewable solvents (EtOAc, 2-methyltetrahydrofuran), thereby eliminating the previously required dipolar aprotic solvent. The copper-catalyzed reaction proceeds with a range of bromobenzaldehydes to give products in good yields. E.g., in presence of CuI and Cs2CO3 under nitrogen in EtOAc, cross-coupling of 2-BrC6H4CHO and Et acetamidoacetate gave 59% indole derivative (I). In addition, the external ligand-free cross-coupling methodol. provides convenient access to an investigational treatment for central nervous system disorders.

ACS Sustainable Chemistry & Engineering published new progress about Cross-coupling reaction. 104291-81-8 belongs to class indole-building-block, name is Ethyl 6-cyano-1H-indole-2-carboxylate, and the molecular formula is C12H10N2O2, Recommanded Product: Ethyl 6-cyano-1H-indole-2-carboxylate.

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

Qin, Hui published the artcileA Mild and Direct C(sp3)-S Cross-Coupling of Oxindoles with Thiols: Synthesis of Unsymmetrical 3-Thiooxindoles, Computed Properties of 71293-59-9, the main research area is thiooxindole preparation coupling oxindole thiol.

Herein, an operationally simple and mild strategy to construct sulfenation of oxindoles with a series of thiols in the absence of transition metals was developed. This methodol. provides an efficient way to directly form a C-S bond at the C-3 position of oxindoles under mild reaction conditions with a cheap and common solvent and base in moderate to good yields.

Journal of Organic Chemistry published new progress about Cross-coupling reaction. 71293-59-9 belongs to class indole-building-block, name is 5,6-Dichloroindolin-2-one, and the molecular formula is C8H5Cl2NO, Computed Properties of 71293-59-9.

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