Tag: 100-200

On March 18, 2004, Chakravarty, Sarvajit; Dugar, Sundeep; Lu, Qing; Luedtke, Gregory R.; Mavunkel, Babu J.; Perumatam, John Joseph; Tester, Richland published a patent.Electric Literature of 256935-86-1 The title of the patent was Preparation of piperidinylcarbonyl- and piperazinylcarbonylindolamines as p38 kinase inhibitors.. And the patent contained the following:

Title compounds [I; 1 Z2 = CA, the other = CR1; R1, R2, R5, R6 = H, noninterfering substituent; A = WiCOXjY; Y = COR2; W, X = spacer of 2-6Å; i, j = 0, 1; 2 R6 may form a 5-6 membered ring; m = 0-4; n = 0-3; L1, L2 = linker; R4 = noninterfering substituent; Z1 = N, CR5; Ar = (substituted) (fused) Ph, thienyl], were prepared for treatment of pro-inflammation response (no data). Thus, 1-(4-fluorobenzyl)-2S,5R-dimethylpiperazine, 6-chloroindole-5-carboxylic acid (preparation given), TBTU, and Et3N were stirred in DMF overnight to give 92% amide, which in CH2Cl2 at 0° was treated with (COCl)2 followed by stirring at room temperature for 5 h. Pyrrolidine was added followed by stirring for 1 h to give 71% 1-[6-chloro-5-[4-(4-fluorobenzyl)-2R,5S-dimethylpiperazine-1-carbonyl]-1H-indol-3-yl]-2-pyrrolidin-1-ylethane-1,2-dione. This was stirred with NaH in THF for 30 min.; O-(diphenylphosphinyl)hydroxylamine was added followed by stirring for 10 h to give 1-[1-amino-6-chloro-5-[4-(4-fluorobenzyl)-2R,5S-dimethylpiperazine-1-carbonyl]-1H-indol-3-yl]-2-pyrrolidin-1-ylethane-1,2-dione. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Electric Literature of 256935-86-1

The Article related to piperidinylcarbonylindolamine piperazinylcarbonylindolamine preparation p38 kinase inhibitor, indolyloxoacetamide amino piperazinylcarbonyl preparation p38 kinase inhibitor, pulmonary sarcosis silicosis cerebral malaria treatment aminoindole preparation, restenosis psoriasis cns reperfusion injury treatment aminoindole preparation and other aspects.Electric Literature of 256935-86-1

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

On October 15, 2021, Ledneczki, Istvan; Horvath, Anita; Tapolcsanyi, Pal; Eles, Janos; Molnar, Katalin Dudas; Vago, Istvan; Visegrady, Andras; Kiss, Laszlo; Szigetvari, Aron; Koti, Janos; Kramos, Balazs; Maho, Sandor; Holm, Patrik; Kolok, Sandor; Fodor, Laszlo; Than, Marta; Kostyalik, Diana; Balazs, Ottilia; Vastag, Monika; Greiner, Istvan; Levay, Gyorgy; Lendvai, Balazs; Nemethy, Zsolt published an article.Product Details of 1609131-18-1 The title of the article was HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor. And the article contained the following:

HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor pos. allosteric modulators. During the hit expansion, several derivatives, such as I-III demonstrated not only high in vitro potency, but also in vivo efficacy in the mouse place recognition test. The advanced hit mol. II was further optimized by the elimination of the putatively mutagenic aromatic-amine building block that resulted in a novel, aminomethylindole compound family. The most balanced physico-chem. and pharmacol. profile was found in case of compound IV. Docking study revealed an inter-subunit binding site to be the most probable for our compounds IV demonstrated favorable cognitive enhancing profile not only in scopolamine-induced amnesia (place recognition test in mice) but also in natural forgetting (novel object recognition test in rats). IV was, furthermore, active in a cognitive paradigm of high translational value, namely in the rat touch screen visual discrimination test. Therefore, IV was selected as a lead compound for further optimization. Based on the obtained favorable results, the invented aminomethylindole cluster may provide a viable approach for cognitive enhancement through pos. allosteric modulation of α7 nAChRs. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Product Details of 1609131-18-1

The Article related to indole allosteric modulator preparation nicotinic acetylcholine receptor cognitive enhancement, highthroughput screening indole allosteric modulator preparation drug discovery, alpha 7 nicotinic acetylcholine receptor, cognitive enhancement, high-throughput screening, positive allosteric modulation, structure-activity relationship and other aspects.Product Details of 1609131-18-1

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

Liu, Tingting; Wu, Kaikai; Wang, Liandi; Yu, Zhengkun published an article in 2019, the title of the article was Potassium tert-butoxide-promoted acceptorless dehydrogenation of N-heterocycles.Category: indole-building-block And the article contains the following content:

Potassium tert-butoxide-promoted acceptorless dehydrogenation of N-heterocycles was efficiently realized for the generation of N-heteroarenes such as quinolines, quinoxalines, indoles, quinazolinones and isoquinolines and hydrogen gas under transition-metal-free conditions. In the presence of KOtBu base, a variety of six- and five-membered N-heterocyclic compounds efficiently underwent acceptorless dehydrogenation to afford the corresponding N-heteroarenes and H2 gas in o-xylene at 140 °C. The present protocol provided a convenient route to aromatic nitrogen-containing compounds and H2 gas. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Category: indole-building-block

The Article related to quinoline quinoxaline indole quinazolinone isoquinoline preparation, tetrahydroquinoline dehydrogenation potassium tert butoxide promoted, tetrahydroquinoxaline dehydrogenation potassium tert butoxide promoted, indoline dehydrogenation potassium tert butoxide promoted, quinazoline dehydrogenation potassium tert butoxide promoted and other aspects.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

On October 26, 2007, Hong, Bor-Cherng; Wu, Ming-Fun; Tseng, Hsing-Chang; Huang, Guo-Fong; Su, Cheng-Feng; Liao, Ju-Hsiou published an article.HPLC of Formula: 79815-20-6 The title of the article was Organocatalytic asymmetric robinson annulation of α,β-unsaturated aldehydes: applications to the total synthesis of (+)-palitantin. And the article contained the following:

Cyclohexadienecarboxaldehydes such as I (R = H, AcO; R1 = H, Me; R2 = AcOCH2, Ph, 2-O2NC6H4, Me, Et, Me2CH) are prepared by enantioselective Robinson annulation reactions of α,β-unsaturated aldehydes (E)-RCH2C(R1):CHCHO [R = H, Me, Et, Me2CH, Ph, 2-O2NC6H4, AcO; R1 = H, Me; RR1 = (CH2)4] in the presence of organic amines such as L-proline or α,α-diphenyl-L-prolinyl and α,α-bis(2-naphthyl)-L-prolinyl trimethylsilyl ethers and in the presence or absence of organic acids or bases. I (R = AcO; R1 = H; R2 = AcOCH2), formed by the stereoselective self-condensation of (E)- or (Z)-AcOCH2CH:CHCHO in the presence of L-proline and triethylamine, is converted in nine steps to (+)-palitantin II. The structure of I (R = H; R1 = Me; R2 = 2-O2NC6H4) is determined by x-ray crystallog.; the absolute configurations of I (R = R1 = H; R2 = Me) and of I (R = H; R1 = Me; R2 = Ph) are determined by their conversion to cyclohexadienecarboxylates of known absolute configuration. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).HPLC of Formula: 79815-20-6

The Article related to cyclohexadienecarboxaldehyde stereoselective enantioselective preparation, palitantin stereoselective enantioselective preparation, organocatalytic stereoselective enantioselective robinson annulation unsaturated aldehyde, organic amine catalyst stereoselective enantioselective robinson annulation unsaturated aldehyde and other aspects.HPLC of Formula: 79815-20-6

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

On January 1, 2018, He, Yi; Li, Zhenghua; Robeyns, Koen; Van Meervelt, Luc; Van der Eycken, Erik V. published an article.HPLC of Formula: 883526-76-9 The title of the article was A Gold-Catalyzed Domino Cyclization Enabling Rapid Construction of Diverse Polyheterocyclic Frameworks. And the article contained the following:

We report herein an efficient gold(I)-catalyzed post-Ugi domino dearomatization/ipso-cyclization/Michael sequence that enables access to libraries of diverse (hetero)arene-annulated tricyclic heterocycles. This process affords novel complex polycyclic scaffolds in moderate to good yields from readily available acyclic precursors with excellent chemo-, regio-, and diastereoselectivity. The power of this strategy has been demonstrated by the rapid synthesis of 40 highly functionalized polyheterocycles bearing indole, pyrrole, (benzo)furan, (benzo)thiophene, pyrazole, and electron-rich arene groups in two operational steps. Thus, e.g., treatment of Ugi adduct I with IPrAuCl/AgOTf afforded polyheterocycle II (96%). The experimental process involved the reaction of 1,5-Dimethyl-1H-indole-2-carbaldehyde(cas: 883526-76-9).HPLC of Formula: 883526-76-9

The Article related to gold catalyzed domino cyclization diverse polyheterocyclic compound synthesis, chemoselective synthesis polyheterocyclic compound, regioselective synthesis polyheterocyclic compound, diastereoselective synthesis polyheterocyclic compound, ugi reaction, dearomatization, domino cyclization, gold catalysis, heterocycles and other aspects.HPLC of Formula: 883526-76-9

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

On October 4, 2021, Luo, Zaoli; Liu, Yungen; Tong, Ka-Chung; Chang, Xiao-Yong; To, Wai-Pong; Che, Chi-Ming published an article.Reference of 6-Chloro-2,3-dihydro-1H-indole The title of the article was Luminescent Platinum(II) Complexes with Bidentate Diacetylide Ligands: Structures, Photophysical Properties and Application Studies. And the article contained the following:

A series of platinum(II) m-terphenyl 2,2”-diacetylide complexes supported by diimines (2,2′-bipyridines, 1,10-phenanthroline, 2,2′-bipyrimidine) or bis-N-heterocyclic carbenes 3-RIm(CH2)nImR-3′ (R = Bu, Me; n = 1-3) ligands have been prepared The diacetylide ligands adopt a cis coordination mode featuring non-planar terphenyl moieties as revealed by X-ray crystallog. analyses. The electrochem., photophys. and photochem. properties of these platinum(II) complexes have been investigated. These platinum(II) diimine complexes show broad emission with peak maxima from 566 nm to 706 nm, with two of them having emission quantum yields >60% and lifetimes <2μs in solutions at room temperature, whereas the platinum(II) diacetylide complexes having bis-N-heterocyclic carbene instead of diimine ligand display photoluminescence with quantum yields of up to 28% in solutions and excited state lifetimes of up to 62μs at room temperature Application studies revealed that one of the complexes can catalyze photoinduced aerobic dehydrogenation of alcs. and alkenes, and a relatively non-toxic water-soluble Pt(II) complex displays anti-angiogenic activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Reference of 6-Chloro-2,3-dihydro-1H-indole

The Article related to platinum diacetylide bipyridine imidazolylidene complex preparation photoluminescence photophysics, crystal structure platinum diacetylide bipyridine imidazolylidene complex, mol structure platinum diacetylide bipyridine imidazolylidene complex, bis-n-heterocyclic carbene, diacetylide, diimine, luminescence, platinum and other aspects.Reference of 6-Chloro-2,3-dihydro-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

Zhong, Jian-Ji; To, Wai-Pong; Liu, Yungen; Lu, Wei; Che, Chi-Ming published an article in 2019, the title of the article was Efficient acceptorless photo-dehydrogenation of alcohols and N-heterocycles with binuclear platinum(II) diphosphite complexes.Application of 52537-00-5 And the article contains the following content:

Binuclear platinum(II) diphosphite complexes as practical and efficient photocatalysts for oxidant-free and acceptorless dehydrogenation of alcs. and N-heterocycles in high yields even under substrate-limiting conditions was described. The reaction could be used for constructing quinazolin-4(3H)-ones from anthranilamide and alcs. This protocol offered the unique reactivity of binuclear platinum(II) diphosphite complexes, wide substrate scope, mild reaction conditions, scalability, utility and versatility of these photocatalysts with practical relevance. Regeneration of the photocatalyst by means of reductive elimination of dihydrogen from the in-situ formed platinum(III)-hydride species represented an alternative paradigm to the current approach in photoredox catalysis. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to binuclear platinum diphosphite complex preparation uv absorption, ketone aldehyde preparation, alc photodehydrogenation binuclear platinum diphosphite complex catalyst, indole quinoline isoquinoline benzothiazole pyrrole preparation, saturated heterocycle photodehydrogenation binuclear platinum diphosphite catalyst and other aspects.Application of 52537-00-5

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

On December 25, 2000, Pasquier, Corinne; Naili, Said; Mortreux, Andre; Agbossou, Francine; Pelinski, Lydie; Brocard, Jacques; Eilers, Juergen; Reiners, Iris; Peper, Viola; Martens, Juergen published an article.Recommanded Product: 79815-20-6 The title of the article was Free and Cr(CO)3-Complexed Aminophosphine Phosphinite Ligands for Highly Enantioselective Hydrogenation of α-Functionalized Ketones. And the article contained the following:

The synthesis and characterization of a new series of aryl- and cycloalkyl-substituted aminophosphine phosphinites, e.g. I (R = cyclopentyl), obtained from the reaction of the three precursors (S)-2-hydroxymethylazetidine, (S)-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline, and (S)-2-hydroxymethylindoline and chlorophosphines is described. The aromatic ring in (S)-2-hydroxymethylindoline has allowed the synthesis and isolation of tricarbonyl chromium complexed amino alcs., which were similarly converted into the corresponding aminophosphine phosphinites, presenting a stereogenic center and a planar chirality. Ligand I ((S)-Cp,Cp-IndoNOP) revealed an unprecedented 31P NMR fluxional behavior related to a rotation inhibition around the P-heteroatom (N and O) bonds. These new AMPP ligands were used in the enantioselective hydrogenation of various α-functionalized ketones, i.e., dihydro-4,4-dimethyl-2,3-furandione 14, N-benzyl benzoylformamide 15, Et pyruvate 16, and 2-(N,N-dimethyl)aminoacetophenone hydrochloride 17. The stereoelectronic effects generated by the presence of the tricarbonyl chromium moiety onto the hydrogenations have been assessed. The beneficial effect of the matching chiralities in ligand associated with the use of the most appropriate nonchiral ligand Cl has resulted in a win of 13% of ee for the rhodium-based hydrogenation of 15. While using the most suitable new chiral AMPP ligand from this study, the four above-mentioned substrates were converted into the corresponding optically active alcs. in >99% ee (14/I), >99% ee (15/I), 87% ee (16/I), and >99% ee (17/I), resp. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Recommanded Product: 79815-20-6

The Article related to chromium complexed aminophosphine phosphinite ligand preparation catalyst enantioselective hydrogenation, functionalized ketone enantioselective hydrogenation catalyst chromium complexed aminophosphine phosphinite, rhodium ruthenium aminophosphine phosphinite complex catalyst enantioselective hydrogenation ketone and other aspects.Recommanded Product: 79815-20-6

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

On August 10, 2006, Jolidon, Synese; Narquizian, Robert; Norcross, Roger, David; Pinard, Emmanuel published a patent.Application of 52537-00-5 The title of the patent was Preparation of heterocyclic substituted phenyl methanones as inhibitors of the glycine transporter 1. And the patent contained the following:

The title compounds I [R1 = halo, cycloalkyl, aryl, etc.; R2 = SO2(alkyl), SO2NH(alkyl), NO2 or CN; het = aromatic or partially aromatic bicyclic amine, which may contain one or two addnl. N-atoms, selected from (un)substituted isoindolyl, indolyl, pyrrolo[3,4-d]pyrimidinyl, etc.], useful for treating illnesses based on the glycine uptake inhibitor, were prepared and formulated. Thus, reacting 2-isopropoxy-5-methansulfonylbenzoic acid (preparation given) with 2,3-dihydro-1H-isoindole afforded 88% II. It has been found that the compounds I are good inhibitors of the glycine transporter 1 (GlyT-1) (IC50 values were given for representative compounds I). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to heterocyclyl phenyl methanone preparation glycine transporter glyt1 inhibitor, isoindolyl phenyl methanone preparation glycine transporter glyt1 inhibitor, indolyl phenyl methanone preparation glycine transporter glyt1 inhibitor, pyrrolopyrimidinyl phenyl methanone preparation glycine transporter glyt1 inhibitor and other aspects.Application of 52537-00-5

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

On February 6, 1986, Henneke, Karl Wilhelm; Wedemeyer, Karlfried published a patent.HPLC of Formula: 52537-00-5 The title of the patent was Procedure for preparing indoline and indoline derivatives. And the patent contained the following:

Indolines I (R1, R2 = H, halo, alkyl, alkoxy; R3 = H, alkyl) were prepared by cyclization of phenethylamines II (X = halo) in the presence of Cu catalysts, characterized in that the cyclization is done in the presence of inorganic carbonates or H carbonates and in the presence of complexing agents for copper ions. Heating a mixture of 2-ClC6H4CH2CH2NH2, CuCl, 8-hydroxyquinoline, soda, and Me2CHCH2OH to boiling and keeping 4-6 h at 120° gave 99.9% pure indoline in 94% yield. Indoline and its derivatives are intermediates for plant protective agents, agrochems., aromas, dyes, and pharmaceuticals. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).HPLC of Formula: 52537-00-5

The Article related to indoline, halophenethylamine cyclization cuprous chelator, plant protective intermediate indoline, agrochem protective intermediate indoline, aroma protective intermediate indoline, dye protective intermediate indoline, pharmaceutical protective intermediate indoline, carbonate cyclization halophenethylamine and other aspects.HPLC of Formula: 52537-00-5

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