Month: October 2022

On December 30, 2004, Howlett, Anthony R.; Rice, Audie; Moshinsky, Deborah; Hammarsten, Ola published a patent.Electric Literature of 52537-00-5 The title of the patent was A preparation of sulfonamide substituted indolinones, useful as inhibitors of DNA dependent protein kinase (DNA-PK). And the patent contained the following:

The invention relates to a preparation of sulfonamide substituted indolinones of formula I [wherein: R1 and R2 are independently selected from H, (un)substituted Ph, thiazolyl, or alkyl, etc.; R3, R4, and R5 are independently selected from H or alkyl], useful as inhibitors of DNA dependent protein kinase (DNA-PK). The invention relates to the field of radiosensitizing agents which are capable of enhancing radiotherapy by inhibiting DNA-PK (DNA-protein kinase). For instance, sulfonamide substituted indolinone II was prepared via condensation of pyrrole derivative III and indole derivative IV. The prepared indolinone derivative V was found to inhibit DNA-PK (IC50 = 1.6 μM). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Electric Literature of 52537-00-5

The Article related to sulfonamide indolinone preparation inhibitor dna dependent protein kinase, pyrrole carboxaldehyde indolone condensation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Electric Literature 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

Wang, Guo-Peng; Chen, Meng-Qing; Zhu, Shou-Fei; Zhou, Qi-Lin published an article in 2017, the title of the article was Enantioselective Nazarov cyclization of indole enones cooperatively catalyzed by Lewis acids and chiral Bronsted acids.SDS of cas: 883526-76-9 And the article contains the following content:

The use of cooperative catalysis using Lewis acids and chiral Bronsted acids to control the stereochem. of the tertiary α-carbon I (R = H, 7-Me, 7-F, 7-Cl, 8-F; R1 = Me, Ph, 2H-1,3-benzodioxol-5-yl, etc.) in the products of this reaction has been reported. Specifically, with ZnCl2 and a chiral spiro phosphoric acid as catalysts, the first enantioselective construction of cyclopenta[b]indoles with chiral tertiary α-carbons I was realized via Nazarov cyclization of indole enone substrates II (R2 = H, 5-Me, 5-F, 5-Cl, 4-F) with only one coordinating site. Mechanistic studies revealed that the chiral spiro phosphoric acid acts as a multifunctional catalyst and it co-catalyzes the cyclization of the dienone and enantioselectively catalyzes a proton transfer reaction of the enol intermediate. This new strategy of enantioselective control by means of cooperative catalysis may show utility for other challenging asym. cyclization reactions. The experimental process involved the reaction of 1,5-Dimethyl-1H-indole-2-carbaldehyde(cas: 883526-76-9).SDS of cas: 883526-76-9

The Article related to cyclopentaindole preparation enantioselective, indole enone nazarov cyclization lewis acid chiral phosphoricacid catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.SDS of cas: 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

Wender, Paul A.; Cooper, Christopher B. published an article in 1986, the title of the article was The photochemistry of 1-alkenylbenzotriazoles. Methodology for the synthesis of indoles.Related Products of 65417-22-3 And the article contains the following content:

Indoles I [R = (CH2)3OSiMe2CMe3, R1 = H; R = H, R1 = (CH2)3OSiMe2CMe3; R = Me, R1 = CO2Me; RR1 = (CH2)3, (CH2)4] were prepared by photolysis of 1-alkenylbenzotriazoles II. The 2,3-dihydropyrrolo[1,2-a]indole nucleus of the mitomycin antitumor antibiotics was prepared by desilylating I [R = (CH2)3OSiMe2CMe3, R1 = H], tosylating the alc., and ring closure of the tosylate. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Related Products of 65417-22-3

The Article related to indole, pyrroloindole mitomycin preparation, alkenylbenzotriazole preparation photolysis, benzotriazole alkenyl photolysis, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Related Products of 65417-22-3

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

On October 11, 2017, Liu, Huan; Chen, Jian-Gang; Wang, Chao; Liu, Zhao-Tie; Li, Yang; Liu, Zhong-Wen; Xiao, Jianliang; Lu, Jian published an article.Product Details of 52537-00-5 The title of the article was Immobilization of Cyclometalated Iridium Complex onto Multiwalled Carbon Nanotubes for Dehydrogenation of Indolines in Aqueous Solution. And the article contained the following:

Increasing concerns about the potentially neg. impacts of chem. production on sustainable development of the overall environment have spurred numerous attempts to seek greener reaction mediums, recyclable catalysts, and high-efficiency procedures. Herein, a cyclometalated Ir complex with a pyrene tag was successfully immobilized onto multiwalled carbon nanotubes via π-π stacking interactions, through which an easily reusable Ir catalyst was constructed. The immobilization process was effectively monitored by using a fluorescence spectroscopy technique, and the immobilized Ir catalyst was well characterized and evaluated. It is found that the immobilized Ir catalyst exerts activity comparable to that of the corresponding homogeneous Ir catalyst for the dehydrogenation of indolines in an aqueous solution More importantly, the catalyst could be recycled seven times without obvious loss of the Ir-active center and noticeable decrease in the yield of the targeted product. Addnl., the observed slight deactivation of the catalyst during the recycle is also discussed. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Product Details of 52537-00-5

The Article related to indoline cyclometalated carbon nanotube immobilized iridium complex dehydrogenation catalyst, indole preparation green chem, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Product Details 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 March 26, 2007, Chen, Yihui; Shibata, Masayuki; Rajeswaran, Manju; Srikrishnan, Thamarapu; Dugar, Sundeep; Pandey, Ravindra K. published an article.HPLC of Formula: 256935-86-1 The title of the article was Utility of Japp-Klingemann reaction for the preparation of 5-carboxy-6-chloroindole via Fischer indole protocol. And the article contained the following:

5-Carboxy-6-chloroindole, a precursor for p38 kinase inhibitor, was prepared from 4-amino-2-chloro-3-iodobenzoic acid by following the Japp-Klingemann synthetic approach. The structures of the key intermediates were also confirmed by X-ray analyses. Computational anal. was helpful in understanding the importance of the substituents at the cyclization step of the synthesis. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to carboxychloroindole preparation japp klingemann reaction, indolecarboxylic acid chloro preparation japp klingemann reaction, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.HPLC of Formula: 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 14, 2004, Nobayashi, Eiji; Fujii, Katsuhiro published a patent.Category: indole-building-block The title of the patent was Preparation of high-purity indolecarboxylic acids from their esters. And the patent contained the following:

Title carboxylic acids are prepared by hydrolysis of their esters I [R1-R6 = H, halo, alkyl, acyl(oxy), alkoxy, aryl, NO2, cyano, etc.; ≥1 of R1-R6 = carboxylic acid ester residue; R7 = H, C1-4 alkyl] with alkali metal hydroxides in nonpolar solvents, H2O, and alcs. Thus, Et 1-methylindole-2-carboxylate was treated with 4.8% aqueous NaOH at 55-59° in MePh and MeOH for 3 h, the organic phase removed, and acidified to give 95% 1-methylindole-2-carboxylic acid with 99.0% purity. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Category: indole-building-block

The Article related to indolecarboxylic acid preparation solvent nonpolar alc water, toluene methanol water solvent hydrolysis indolecarboxylate ester, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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 July 28, 2005, Baldwin, Ian Robert; Bamborough, Paul; Christopher, John Andrew; Kerns, Jeffrey K.; Longstaff, Timothy; Miller, David Drysdale published a patent.Name: Methyl 5-bromoindoline-7-carboxylate The title of the patent was Preparation of 7-indolecarboxamides as IKK2 kinase inhibitors for the treatment of such as inflammatory and tissue repair disorders. And the patent contained the following:

Title compounds I [wherein R1, R2 = H, halo, alkylene, alkenylene, (hetero)aryl, etc., and salts, solvates, or physiol. functional derivatives thereof] were prepared as IKK2 kinase inhibitors. For instance, Pd-catalyzed coupling of Boc-protected bromide II (preparation given) with phenylboronic acid followed by deprotection with HCl gave 7-indolecarboxamide III. Most invented compounds were found to have activity >4.8 in the IKK2 assay, in which the degree of phosphorylation of GST-IκBα was measured as a ratio of specific 665 nm energy transfer signal to reference europium 620 nm signal. Therefore, I and their pharmaceutical compositions are useful in the treatment and prevention of disease states mediated by IKK2 mechanisms, including inflammatory and tissue repair disorders. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).Name: Methyl 5-bromoindoline-7-carboxylate

The Article related to indolecarboxamide preparation ikk2 kinase inhibitor, treatment inflammatory tissue repair disorder indolecarboxamide preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Name: Methyl 5-bromoindoline-7-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

On February 15, 2012, Lin, Ning; Luo, Ren-shi; Chen, Miao-miao; Lu, Gui published an article.COA of Formula: C9H9NO2 The title of the article was Synthesis and characterization of two chiral indoline derivatives. And the article contained the following:

Two indoline carboxylic acid derivatives (S)-(1-methylindolin-2-yl)diphenylmethanol and (S)-2-(1-methylindolin-2-yl)-1,3-diphenylpropan-2-ol were synthesized from (S)-indoline-2-carboxylic acid, through the N-methylation, esterification and Grignard addition The total yields of the two products were 86.5% and 89.7% resp. The structures of product were confirmed by 1HNMR, 13CNMR and HRMS. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).COA of Formula: C9H9NO2

The Article related to chiral indolinecarboxylic acid methylation esterification addition, methylindolinyl diphenylmethanol diphenylpropanol preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C9H9NO2

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 November 30, 1977, Bergman, Jan; Carlsson, Rene; Sjoberg, Birger published an article.Safety of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was The reaction of indole and the indole Grignard reagent with phosgene. A facile synthesis of indole-3-carboxylic acid derivatives. And the article contained the following:

Indole-3-carboxylic and indole-3-glyoxylic acid derivatives were prepared from indoles or oxindoles and phosgene or oxalyl chloride. In this reaction, the indole Grignard reagent gave several products, including the cyclotetramers I (X = CO, COCO). Indolo-fused heterocycles were also prepared by this reaction. Thus, phosgene and 2-(2-hydroxyphenyl)-N-methylindole gave 5,6-dihydro-11-methyl-6-oxobenzo[a]pyrano[4,3-b]indole (II). The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Safety of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to indole reaction phosgene, oxindole reaction phosgene, oxalyl chloride reaction indole, grignard indole phosgene, benzopyranoindole, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Safety of Methyl 2-methyl-1H-indole-3-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

On July 12, 2022, Hou, Wei; Dong, Hewei published a patent.Category: indole-building-block The title of the patent was Green preparation method of off-DNA and on-DNA arylselenyl indole compounds and its applications. And the patent contained the following:

The present invention relates to the green preparation method of off-DNA and on-DNA arylselenyl indole compounds and its applications. In particular, preparation method comprises of indole compounds, benzisoselenazolone compounds and the Lewis acid are dissolved in a solvent, and the reaction is stirred for 1 to 12 h at -20 to 65°C, to obtain 3-arylselenoindole compounds I (wherein, R1 is selected from hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, halogen, C1-C4 alkoxy, C1-C4 haloalkoxy, etc.; R2 is selected from hydrogen, C1-C4 alkyl, unsubstituted or halogenated, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4alkoxy, etc.; R3 is selected from the one in hydrogen, halogen, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl, C1-C4 haloalkyl, nitro, carboxyl, C1-C4 alkoxycarbonyl; R4 is selected from hydrogen, C3-C8 cycloalkyl, unsubstituted or halogenated, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, etc.). Similarly, preparation method of on-DNA arylselenyl indole compounds comprises of on-DNA indole compounds, benzisoselenazolone compounds and the Lewis acid are dissolved in a solvent to construct a reaction system, react at 15-50°C for 0.5 to 24 h, the gained reaction solution is after post-processing, obtain compounds II (R5 consists of 0-10 atoms, when the skeleton of R5 consists of 0 atoms, the carbonyl group is directly connected to the indolyl group; when the skeleton of R5 consists of 1-10 atoms, the group is any one of the -CH2-, CF2-, -CH2-O-, etc.; R6 is selected from a kind of in hydrogen, halogen, C1-C6 alkyl,nitro, etc.; R7 is selected from hydrogen, one of C1-C6 alkyl, C1-C6 haloalkyl, Ph, etc.; R8 is selected from hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, halogen, C1-C6 alkoxy group etc.; R9 is selected from hydrogen, C6-C10 aryl, C1-C6 alkyl, etc.). The inventive method has advantages of only needs to add catalytic amount of lewis acid catalyst, the catalyst is cheap and easy to get, simple reaction system, the reaction is to air and water tolerance, doesn’t need inert gas protection, the reaction solvent without removing water, easy to operate; reaction condition is gentle, reaction yield is high and has excellent functional group tolerance; this synthetic method is also applicable to synthesis of porous plate parallel; product is single, and the organic solvent/water mixed phase to carry out, the operation is simple, does not introduce metal reagent, environment friendly, it is applicable to use a perforated plate for the DNA encoding the synthesis of compound library. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Category: indole-building-block

The Article related to arylselenyl indole green preparation selenization antitumor agent, dna conjugated arylselenyl indole green preparation selenization, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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