Day: November 18, 2022

Nguyen, Sierra C. published the artcileSynthesis of semi-saturated polycyclic 1,2,4-triazoles from lactams, Product Details of C8H7NO2, the main research area is polycyclic triazole preparation; lactam hydroxylamine sulfonic acid amination ethyl ethoxy iminoacetate condensation.

A two-step method for the preparation of annulated 1,2,4-triazoles has been developed via the hydroxylamine-O-sulfonic acid (HOSA)-mediated N-amination of readily available lactams followed by condensation with Et 2-ethoxy-2-iminoacetate. Various annulated ring sizes can be incorporated into the resulting polycyclic triazoles.

Tetrahedron Letters published new progress about Amination. 366453-21-6 belongs to class indole-building-block, name is 4-Hydroxy-2,3-dihydroisoindol-1-one, and the molecular formula is C8H7NO2, Product Details of C8H7NO2.

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

Corrieri, Matteo published the artcilePractical and sustainable preparation of pyrrolo[2,3-b]indoles by Cu/Fe catalyzed intramolecular C(sp2)-H amination, Name: 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is pyrrolo indole copper iron catalyzed intramol amination.

A practical, robust and chemoselective approach toward the synthesis of pyrrolo[2,3-b]indoles via direct intramol. C-H bond amination of α-indolylhydrazones has been achieved. This base- and oxidant-free chemoselective transformation relies on a Cu/Fe co-catalyst system that operates at 50 °C in air with water as the only reaction medium. The easy product isolation together with the recyclable catalyst aqueous system (reused at least five times, maintaining over 50% of its catalytic activity) can provide an effective environmentally benign approach to fused N-heterocycles of remarkable interest in pharmaceutical and medicinal chem. The ability of the hydrazone residue to act as a chelating/directing group as well as an aminating agent guarantees the success of this C-H functionalization.

Green Chemistry published new progress about Amination. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Name: 4-(Benzyloxy)-1-methyl-1H-indole.

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, Qixue published the artcileVisible-Light-Promoted Redox Neutral C-H Amidation of Heteroarenes with Hydroxylamine Derivatives, Name: 4-(Benzyloxy)-1-methyl-1H-indole, the main research area is iridium photocatalyst amidation heteroarene hydroxylamine derivative.

A room temperature redox neutral direct C-H amidation of heteroarenes has been achieved. Hydroxylamine derivatives, which are easily accessed, have been employed as tunable nitrogen sources. These reactions were enabled by a visible-light-promoted single-electron transfer pathway without a directing group. A variety of heteroarenes, such as indoles, pyrroles, and furans, could go through this amidation with high yields (up to 98%). E.g., irradiation of N-methylindole, TsONTsMe, the photocatalyst fac-Ir(ppy), and NaHCO3 in DMF gave 66% amide (I). These reactions are highly regioselective, and all the products were isolated as a single regioisomer.

Organic Letters published new progress about Amidation. 13523-93-8 belongs to class indole-building-block, name is 4-(Benzyloxy)-1-methyl-1H-indole, and the molecular formula is C16H15NO, Name: 4-(Benzyloxy)-1-methyl-1H-indole.

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

Harrison, Darwin Anil published the artcileSynthesis and antifungal activity of 1-aminomethyl-3-(p-tolylthiosemicarbazono)-4,5/5,6-dichloroindolin-2-ones, Synthetic Route of 1677-47-0, the main research area is thiosemicarbazide indolinedione amine formaldehyde condensation Mannich aminomethylation; aminomethyl thiosemicarbazonoindolinone preparation antifungal.

P-Tolylthiosemicarbazide on condensation with 4,5/5,6-dichloroindoline-2,3-diones gave 3-(p-tolylthiosemicarbazono)-4,5/5,6-dichloroindolin-2-ones which on aminomethylation with secondary amines in the presence of formaldehyde gave 1-aminomethyl-3-(p-tolylthiosemicarbazono)-4,5/5,6-dichloroindolin-2-ones. The compounds were screened for their antifungal potential against human pathogenic fungi and their structures were elucidated with the help of elemental anal. and spectral data (1H NMR and Mass).

Indian Journal of Heterocyclic Chemistry published new progress about Fungicides. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, Synthetic Route 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

Pellicciari, Roberto published the artcileOn the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives, Safety of 4-Hydroxy-2,3-dihydroisoindol-1-one, the main research area is excitotoxins cell death PARP2 inhibitor isoquinoline derivative SAR preparation.

PARP-1 and PARP-2 are members of the family of poly(ADP-ribose)polymerases, which are involved in the maintenance of genomic integrity under conditions of genotoxic stimuli. The different roles of the two isoforms under pathophysiol. conditions have not yet been fully clarified, and this is partially due to the lack of selective inhibitors. We report herein the synthesis and preliminary pharmacol. evaluation of a large series of isoquinolinone derivatives as PARP-1/PARP-2 inhibitors. Among them, we identified the 5-benzoyloxyisoquinolin-1(2H)-one derivative as the most selective PARP-2 inhibitor reported so far, with a PARP-2/PARP-1 selectivity index greater than 60.

ChemMedChem published new progress about Cell death. 366453-21-6 belongs to class indole-building-block, name is 4-Hydroxy-2,3-dihydroisoindol-1-one, and the molecular formula is C8H7NO2, Safety of 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

Bien, Jeffrey published the artcileThe First Kilogram Synthesis of Beclabuvir, an HCV NS5B Polymerase Inhibitor, Recommanded Product: 3-Cyclohexyl-1H-indole-6-carboxylic acid, the main research area is beclabuvir diastereoselective enantioselective kilogram scale preparation; stereoselective rhodium catalyzed cyclopropanation alkylation key step preparation beclabuvir; palladium catalyzed intramol arylation key step preparation beclabuvir.

A process for the multikilogram-scale preparation of the hepatitis B NS5B RNA polymerase inhibitor beclabuvir I was developed using a diastereoselective and enantioselective cyclopropanation using the Davies catalyst Rh2(S-DOSP)4, an alkylation to merge indole and cyclopropane fragments, and an intramol. palladium-catalyzed arylation as the key steps. I·HCl was prepared in 12 linear steps with 5 isolations in an overall yield of 8%.

Organic Process Research & Development published new progress about Alkylation. 494799-17-6 belongs to class indole-building-block, name is 3-Cyclohexyl-1H-indole-6-carboxylic acid, and the molecular formula is C15H17NO2, Recommanded Product: 3-Cyclohexyl-1H-indole-6-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

Dutt, Rohit published the artcileImproved superaugmented eccentric connectivity indices – Part II: Application in development of models for prediction of hiCE and hCE1 inhibitory activities of isatins, Category: indole-building-block, the main research area is carboxylesterase liver intestine superaugmented eccentric connectivity topochem index.

Topochem. versions of all the four superaugmented eccentric connectivity indexes (denoted by: SAcξ4c, SAcξ5c, SAcξ6c, and SAcξ7c) were utilized for the development of models for prediction of hiCE and hCE1 inhibitory activities. The values of these topochem. indexes were computed for each of the 65 analogs constituting the data set using an inhouse computer program. Resulting data was analyzed and suitable models were developed after identification of the active ranges by maximization of moving average with regard to active derivatives Subsequently, two biol. activities were assigned to each analog using proposed models, which were then compared with the reported hiCE and hCE1 inhibitory activities. Statistical significance of topol. indexes/models was investigated through sensitivity, specificity, and Matthews correlation coefficient (MCC). The overall accuracy of prediction varied from a min. of 81% for a model based upon SAcξ4c to a maximum of 92% in case of a model based upon SAcξ5c with regard to hiCE inhibitory activity and from a min. of 85% for a model based upon SAcξ4c to a maximum of 94% in case of a model based upon SAcξ7c with regard to hCE1 inhibitory activity. An excellent relationship between new generation superaugmented eccentric connectivity topochem. indexes (SAcξ4c, SAcξ5c, SAcξ6c, and SAcξ7c) and hiCE and hCE1 inhibitory activities can be attributed to the sensitivity of the proposed topol. indexes toward nature, number, and relative position of heteroatom. High predictability amalgamated with high potency of the active ranges offer proposed models a vast potential for providing lead structures for development of potent and selective hiCE and hCE1 inhibitors.

Medicinal Chemistry Research published new progress about Drug design. 1677-47-0 belongs to class indole-building-block, name is 4,5-Dichloroisatin, and the molecular formula is C8H3Cl2NO2, Category: 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

McDonald, Brian G. published the artcileConversion of (2-chlorallyl)amines into heterocyclic compounds. I. 2-Methylindoles, 1,5,6,7-tetrahydro-3-methylindol-4-ones, and related heterocycles, Formula: C11H11NO2, the main research area is cyclization aniline chloroallyl 231; indole methyl; oxazoloquinoline; imidazopyridine; pyrroloquinoline.

The allylanilines I [R = H, Me, (CH2)2CO2Me, R1 = H; R = H, R1 = 2-Ph, 2-CO2Me, 3-Me, 4-Cl, 4-Me, 4-CO2Me], prepared by condensation of R1C6H4NHR with CH2:CClCH2R2 (R2 = Cl, I), gave 5-75% II on heating with polyphosphoric acid at 100° or BF3-MeOH at 150°. This method was used for the preparation of other heterocyclic compounds e.g. condensation of 4,7-dichloroquinoline with R3NHCH2CCl:CH2 (R3 = Ph, Et) and cyclization of the product formed gave 30-42% pyrroloquinolines III.

Journal of the Chemical Society, Perkin Transactions 18: Organic and Bio-Organic Chemistry published new progress about Cyclization. 57663-18-0 belongs to class indole-building-block, name is Methyl 2-methyl-1H-indole-5-carboxylate, and the molecular formula is C11H11NO2, Formula: C11H11NO2.

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

Bakke, Jan published the artcileNew syntheses of substituted indoles, SDS of cas: 41910-64-9, the main research area is indole chloro phenyl; phenethyl chloride nitro cyclization; cyclization nitrophenethyl chloride.

The indoles I (R = H, 4-Cl, 6-Cl, 4-NH2) were prepd by cyclizing RC6H3(CH2CH2Cl)(NO2)-1,2 (R = H, 6-Cl, 4-Cl, 6-O2N) with Fe and dehydration of the resulting dehydroindole with Pd/C. o-O2NC6H4Me was condensed with PhCHO to give o-O2NC6H4CH2(O)HPh which was oxidized with concentrated HNO3 and the product cyclized by catalytic reduction to give 2-phenylindole.

Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry published new progress about Cyclization. 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

Ito, Yoshihiko published the artcileIndole syntheses with o-tolyl isocyanide. 3-Acylindoles and 2-substituted indoles, Safety of 2-(tert-Butyl)-5-chloro-1H-indole, the main research area is indole acyl; tolyl isocyanide acylation; cyclization acylmethylphenyl isocyanide.

o-(Lithiomethyl)phenyl isocyanide, generated from o-tolyl isocyanide and (Me2CH)2NLi in diglyme, reacts with allyl esters to produce o-(acylmethyl)phenyl isocyanides. Similarly, acylation of 4-chloro-2-methylphenyl isocyanide, 2,4-dimethylphenyl isocyanide, and 2,6-dimethylphenyl isocyanide produces the corresponding o-(acylmethyl)phenyl isocyanides in moderate yields. o-(Acylmethyl)phenyl isocyanides are heated with Cu2O catalyst in benzene to give 3-acylindole. o-(Acylmethyl)phenyl isocyanides are hydrolyzed to afford 2-alkyl(or 2-aryl)indoles.

Journal of Organic Chemistry published new progress about Cyclization. 69622-40-8 belongs to class indole-building-block, name is 2-(tert-Butyl)-5-chloro-1H-indole, and the molecular formula is C12H14ClN, Safety of 2-(tert-Butyl)-5-chloro-1H-indole.

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