Day: November 17, 2022

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

Masters, Kye-Simeon published the artcileortho-Bromo(propa-1,2-dien-1-yl)arenes: Substrates for domino reactions, Application of Methyl 2-methyl-1H-indole-5-carboxylate, the main research area is indole preparation; bromopropadienylarene amine amide domino reaction Pd catalyst.

O-Bromo(propa-1,2-dien-1-yl)arenes exhibit novel and orthogonal reactivity under Pd catalysis in the presence of secondary amines to form enamines (concerted Pd insertion, intramol. carbopalladation, and terminative Buchwald-Hartwig coupling) and of amides to form indoles (addition, Buchwald-Hartwig cyclization, and loss of the acetyl group). The substrates for these reactions can be accessed in a reliable and highly selective two-step process from 2-bromoaryl bromides.

Journal of Organic Chemistry published new progress about Addition reaction. 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Application of Methyl 2-methyl-1H-indole-5-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

Wang, Pei-Long published the artcilePalladium-Catalyzed C-7 Selective C-H Carbonylation of Indolines for Expedient Synthesis of Pyrroloquinazolinediones, Safety of 4-Chloroindoline, the main research area is pyrroloquinazolinedione preparation; carbon monoxide carbonylation indoline palladium catalyst.

A novel palladium-catalyzed C-7 selective C-H carbonylation of indolines with carbon monoxide for an expedient synthesis of pyrroloquinazolinediones, a structural motif with great potential in biol. active compounds, has been developed. Oxidation of the pyrroloquinazolinedione with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) could easily afford the corresponding indole-based derivative in excellent yield.

Advanced Synthesis & Catalysis published new progress about C-H bond activation. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Safety of 4-Chloroindoline.

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

Jiang, Xinpeng published the artcileFlavin/I2-Catalyzed Aerobic Oxidative C-H Sulfenylation of Aryl-Fused Cyclic Amines, Name: 4-Chloroindoline, the main research area is flavin iodine catalyst oxidative sulfenylation aryl fused cyclic amine.

We report an aerobic oxidative C-H sulfenylation of aryl-fused cyclic amines with various thiols catalyzed by flavin/I2 for the first time. While flavin I catalyzed the C-H sulfenylation of indolines to afford 3-sulfenylindoles, flavin II enabled transformations resulted in substitution at the position para to the N atom on the aryl ring to obtain 6-sulfenylquinolines. The advantages of this metal-free oxidative C-S coupling approach utilizing ambient oxygen as the terminal oxidant were that it was conducted under mild conditions with good atom-efficiency and excellent functional compatibility.

European Journal of Organic Chemistry published new progress about C-H bond activation. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Name: 4-Chloroindoline.

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

Sato, Kenjiro published the artcileDiscovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists, COA of Formula: C8H8ClN, the main research area is indoline carbamate indolinylpyrimidine preparation GPR119 agonist; Conformation; GPCR; GPR119 agonist; Indoline; Type 2 diabetes mellitus.

GPR119 has emerged as an attractive target for antidiabetic agents. The authors identified a structurally novel GPR119 agonist that carries a 5-(methylsulfonyl)indoline motif as an early lead compound To generate more potent compounds of this series, structural modifications were performed mainly to the central alkylene spacer. Installation of a carbonyl group and a Me group on this spacer significantly enhanced agonistic activity, resulting in the identification of I. To further expand the chem. series of indoline-based GPR119 agonists, several heterocyclic core systems were introduced as surrogates of the carbamate spacer that mimic the presumed active conformation. This approach successfully produced an indolinylpyrimidine II, which has potent GPR119 agonist activity. In rat oral glucose tolerance tests, these two indoline-based compounds effectively lowered plasma glucose excursion and glucose-dependent insulin secretion after oral administration.

Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, COA of Formula: C8H8ClN.

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

Yao, Chun-Hsu published the artcileDiscovery of Novel N-β-D-Xylosyl-indole Derivatives as Sodium-Dependent Glucose Co-transporter 2 (SGLT2) Inhibitors for the Management of Hyperglycemia in Diabetes, SDS of cas: 41910-64-9, the main research area is aryl C glycoside preparation antidiabetic; human xyloside indole SGLT2 inhibitor hyperglycemia diabetes antidiabetic preparation.

A novel series of N-linked β-D-xylosides were synthesized and evaluated for inhibitory activity against sodium-dependent glucose co-transporter 2 (SGLT2) in a cell-based assay. Of these, the β-D-xylopyranosyl-1H-indole I (R = 4-chlorocyclopropylbenzyl) was the most potent inhibitor, with an EC50 value similar to that of the natural SGLT2 inhibitor phlorizin. Further studies in Sprague-Dawley (SD) rats indicated that I significantly increased urine glucose excretion in a dose-dependent manner with oral administration. The antihyperglycemic effect of I was also observed in streptozotocin (STZ) induced diabetic SD rats. These results described here are a good starting point for further investigations into N-glycoside SGLT2 inhibitors.

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, SDS of cas: 41910-64-9.

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

Zhang, Hailong published the artcileConstruction of the N1-C3 Linkage Stereogenic Centers by Catalytic Asymmetric Amination Reaction of 3-Bromooxindoles with Indolines, Product Details of C8H8ClN, the main research area is nickel catalyst asym amination bromooxindole indoline.

The catalytic asym. amination reaction of 3-bromooxindoles with indolines for the construction of the N1-C3 linkage stereogenic centers has been realized for the first time. E.g., in presence of Ni(OAc)2, ligand (I), and DABCO in MTBE, amination of 3-bromooxindole derivative (II) with indoline gave 87% III. Moreover, the racemic substrates (3-substituted indolines) were also applicable under the same chiral conditions. The newly developed method conveniently led to a formal synthesis of (+)-psychotrimine.

Organic Letters published new progress about Amination catalysts. 41910-64-9 belongs to class indole-building-block, name is 4-Chloroindoline, and the molecular formula is C8H8ClN, Product Details of C8H8ClN.

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

Vangveravong, Suwanna published the artcileSynthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626, Recommanded Product: N,N-Dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-3-yl)methanamine, the main research area is dopamine D2 receptor antagonist indole benzofuran benzothiophene preparation SAR.

A series of indole, 7-azaindole, benzofuran, and benzothiophene compounds have been prepared and evaluated for affinity at D2-like dopamine receptors. These compounds share structural elements with the classical D2-like dopamine receptor antagonists haloperidol, N-methylspiperone and benperidol. Two new compounds, 4-(4-iodophenyl)-1-((4-methoxy-1H-indol-3-yl)methyl)piperidin-4-ol (6) and 4-(4-iodophenyl)-1-((5-methoxy-1H-indol-3-yl)methyl)piperidin-4-ol (7), were found to have high affinity to and selectivity for D2 vs. D3 receptors. Changing the aromatic ring system from an indole to other heteroaromatic ring systems reduced the D2 binding affinity and the D2 vs. D3 selectivity.

Bioorganic & Medicinal Chemistry published new progress about Dopamine antagonists. 5654-92-2 belongs to class indole-building-block, name is N,N-Dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-3-yl)methanamine, and the molecular formula is C10H13N3, Recommanded Product: N,N-Dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-3-yl)methanamine.

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

Fu, Li Qiang published the artcileSynthesis and antibacterial activity of pleuromutilin derivatives with novel C(14) side chain, Recommanded Product: 4-Hydroxy-2,3-dihydroisoindol-1-one, the main research area is pleuromutilin derivative synthesis antibacterial agent.

In order to find novel antibacterial agents with superior antibacterial activity and overcoming multidrug resistance, a series of pleuromutilin derivatives with novel C(14) side chain were synthesized and evaluated for their in vitro antibacterial activities. The results of antibacterial activities indicated that most of the derivatives showed potent activities against Gram-pos. organisms. In particular, compound I exhibited the most potent inhibitory activity compared with pleuromutilin and linezoid, emerged as potential mol. for further investigation.

Chinese Chemical Letters published new progress about Antibacterial agents. 366453-21-6 belongs to class indole-building-block, name is 4-Hydroxy-2,3-dihydroisoindol-1-one, and the molecular formula is C8H7NO2, Recommanded Product: 4-Hydroxy-2,3-dihydroisoindol-1-one.

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

Zheng, Xudong published the artcileSynthesis of substituted tryptanthrin via aryl halides and amines as antitumor and anti-MRSA agents, Related Products of indole-building-block, the main research area is tryptanthrin derivative synthesis aryl halide amine antitumor anti MRSA.

The natural alkaloid, tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione, I), and its analogs are found to exhibit potent antitumor and anti-MRSA activities. An efficient and convenient method has been developed for the synthesis of tryptanthrin D-ring derivatives through the reaction of substituted tryptanthrins and secondary amines in moderate to good yields. Some of the new compounds exhibited antitumor activities against the human tumor cell lines A549, HCT116 and MDA-MB-231, with mean IC50 values at low micromolar levels. In addition, some of the compounds showed excellent anti-MRSA activities and were more effective than vancomycin, with MIC values of 0.31-1.25 μg/mL for Mu50,RN4220, and Newman strains.

Tetrahedron published new progress about Antibacterial agents. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, 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