Day: October 31, 2022

Das, Krishna Kanta; Ghosh, Asim Kumar; Hajra, Alakananda published an article in 2022, the title of the article was Late-stage ortho-C-H alkenylation of 2-arylindazoles in aqueous medium by Manganese(I)-catalysis.Synthetic Route of 79815-20-6 And the article contains the following content:

Earth-abundant and water-tolerant manganese(I) catalyzed alkenylation of 2-arylindazoles I (R = H, F, Cl; R1 = H, 4-Me, 3-Cl, etc.) with alkyl and aryl alkynes R2CCR3 (R2 = H, Ph, Me; R3 = hexyl, Ph, thiophen-3-yl, etc.) through C-H bond activation is described with a unique level of E-selectivity. The reaction proceeds through the control of C3 nucleophilicity of 2-aryl indazoles. This method is applied to the late-stage functionalization of complex mols. including ethinylestradiol, norethisterone, and N-protected amino acid derivatives, e.g., prop-2-yn-1-yl (tert-butoxycarbonyl)-L-phenylalaninate. The kinetic isotope studies suggest that the C-H bond activation step may not be the rate-determining step. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Synthetic Route of 79815-20-6

The Article related to aryl indazole alkenyl preparation diastereoselective regioselective, alkyne aryl indazole alkenylation manganese catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Synthetic Route of 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 October 26, 2012, Woolford, Alison Jo-Anne; Howard, Steven; Buck, Ildiko Maria; Chessari, Gianni; Johnson, Christopher Norbert; Tamanini, Emiliano; Day, James Edward Harvey; Chiarparin, Elisabetta; Heightman, Thomas Daniel; Frederickson, Martyn; Griffiths-Jones, Charlotte Mary published a patent.Electric Literature of 52537-00-5 The title of the patent was Preparation of bicyclic heterocycles as anticancer agents. And the patent contained the following:

The invention relates to bicyclic heterocycles of formula I and tautomeric and stereochem. isomeric forms, N-oxides, pharmaceutically acceptable salts and the solvates thereof as anticancer agents; their preparation and use in the treatment of cancer. Compounds of formula I wherein ring E is a 6-membered aromatic carbocyclyl and heterocyclyl; G and J are independently C and N; Q is CR and N; R1 is (un)substituted C1-4 alkyl, C2-4 alkenyl and C3-8 cycloalkyl; R2 and R4 are independently (un)substituted H, C1-6 alkyl, C2-6 alkenyl, etc.; R2 and R4 together with the carbon attached form 3- to 10-membered saturated carbocyclyl and heterocyclyl; R3 and R10 are independently (un)substituted H, C1-6 alkyl, C2-6 alkenyl, etc.; R2 and R4 together with the carbon attached form 3- to 10-membered saturated carbocyclyl and heterocyclyl; R is (un)substituted C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, etc.; and tautomeric and stereochem. isomeric forms, N-oxides, pharmaceutically acceptable salts and the solvates thereof, are claimed. Example compound II was prepared by BOC-deprotection of (R)-2-methyl-4-[2-6-methylsulfamoyl-2,3-dihydroindol-1-yl)-2-oxo-ethyl]piperazine-1-carboxylic acid tert-Bu ester. All the invention compounds were evaluated for their antiproliferative activity (some data given). 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 bicyclic heterocycle preparation anticancer agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) 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

On November 30, 2008, Jainta, Manuel; Nieger, Martin; Brase, Stefan published an article.Application In Synthesis of H-Idc-OH The title of the article was Microwave-assisted stereoselective one-pot synthesis of symmetrical and unsymmetrical 2,5-diketopiperazines from unprotected amino acids. And the article contained the following:

The facile condensation of unprotected amino acids by phosphite-promoted one-step coupling reaction is a highly efficient synthesis to generate stereoselective and optically pure sym. and unsym. functionalized diketopiperazines. The use of microwaves enhanced by small amounts of ionic liquid is accompanied by significant improvement in reaction times and yields. Simple filtration through a pad of silica provides the pure compounds in very good to excellent yields. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Application In Synthesis of H-Idc-OH

The Article related to diketopiperazine derivative preparation, amino acid cyclization, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application In Synthesis of H-Idc-OH

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 2, 2018, Huang, Qi; Zard, Samir Z. published an article.Related Products of 65417-22-3 The title of the article was Inexpensive Radical Methylation and Related Alkylations of Heteroarenes. And the article contained the following:

A simple method for the introduction of a Me and higher aliphatic group to various heteroarenes using very inexpensive reagents is described. It is based on the radical addition of a carboxylic xanthate followed by decarboxylation. Depending on the heteroarene structure, the decarboxylation can be spontaneous or induced by heating in N,N-dimethylacetamide or N-Me pyrrolidone in a microwave oven. 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 heteroarene radical alkylation, alkylated heteroarene preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) 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 May 17, 2012, Cheng, Clifford; Shipps, Gerald W., Jr.; Huang, Xiaohua; Huang, Ying; Shao, Ning; Rao, Ashwin; Palani, Anandan; Orth, Peter; Voigt, Johannes H.; Herr, Robert J.; Rossiter, Lana Michele; Zeng, Qi; Sun, Xianfeng published a patent.Application of 52537-00-5 The title of the patent was Preparation of heterocyclic inhibitors of fatty acid binding protein for use in therapy. And the patent contained the following:

The present invention relates to novel heterocyclic compounds of general formula I (wherein each of X, Y, and Z is C or N; R1 is H, halo, CN, etc.; R2 is OH, halo, C1-6alkyl, etc.; one of R3 and R4 is H or C1-6alkyl, and the other is, e.g., heteroaryl(Ra)3; Ra is H, halo, OH, etc.; or R3 and R4 together are part of a 4-7-membered ring) as Fatty Acid Binding Protein (“”FABP””) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity, or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from 6,7-difluoro-3-hydroxyquinoxaline-2-carboxylic acid and racemic-2-(3-chlorobenzyl)pyrrolidine, had a TdF Kd value of 0.08 μM in an assay to demonstrate FABP inhibitory activity. 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 heterocyclic inhibitor fatty acid binding protein preparation therapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) 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 March 2, 2016, Zhong, Wenhe; Jin, Chuanfei; Zhang, Yingjun; Zhang, Ji published a patent.Reference of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of indoline derivatives for treating or preventing diseases related with 5-HT6 receptor. And the patent contained the following:

The invention relates to indoline derivatives (e.g., I), their stereoisomers, tautomers, nitrogen oxides, solvates, metabolites and pharmaceutically acceptable salts, and prodrugs thereof, processes for preparing them, pharmaceutical preparations comprising them, and their use for treating or preventing diseases related with 5-HT6 receptor. For instance, the invention compound I was prepared and gave a 5-HT6 Ki value of 57 nM. 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 indoline preparation hydroxytryptamine gastrointestinal antiobesity cns, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) 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

On July 24, 2014, Buckman, Brad Owen; Nicholas, John Beamond; Emayan, Kumaraswamy; Seiwert, Scott D.; Yuan, Shendong published a patent.Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate The title of the patent was N-Heteroaryl carbamates as lysophosphatidic acid receptor antagonists and their preparation. And the patent contained the following:

Compounds of formula I, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. Compounds of formula I wherein one of and B is acetylene and the other is (un)substituted 6- to 11-membered aryl, (un)substituted 5- to 11- membered heteroaryl, (un)substituted 4- to 11-membered heterocyclyl and (un)substituted 4- to 11-membered carbocyclyl; G is (un)substituted 6- to 11-membered aryl, (un)substituted 5- to 11- membered heteroaryl, (un)substituted 5- to 11-membered heterocyclyl and (un)substituted 5- to 11-membered carbocyclyl; D is OH, CO2H and derivatives, CONH2 and derivatives, azolyl, etc.; E is (un)substituted 6- to 10-membered arylene, (un)substituted 3- to 11-membered carbocyclyl, (un)substituted 3- to 11-membered heterocyclyl and (un)substituted 5- to 10-membered heteroarylene; J is (CR4R5)0-3; K is (CR2’R3′)n; M is (CR2R3)m; n and m are independently 0 – 3, provided that the sum of m + n is equal or greater than 1; L1 and L2 are independently a bond, CH2, CC, etc.; L3 is azolyl, thienyl, aminosulfonyl, etc.; L5 is single bond, CH=CH, CC, etc.; dashed bonds are single and double bonds; each Y is independently absent CR9, C(R9)2, N and NH, provided that only one of Y can be absent; R2, R2′, R3 and R3′ are independently H, halo, alkyl, haloalkyl, etc.; R4, R5 and R9 are independently H and (un)substituted alkyl; R4R5 or two adjacent R9 can be taken together to form (un)substituted cycloalkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their LPA antagonistic activity. From the assay, it was determined that compound II exhibited EC50 value in the range of greater than or equal to 50 nM and less than or equal to 500 nM. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate

The Article related to heteroaryl carbamate preparation lysophosphatidic acid receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate

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, 2000, Mavunkel, Babu J.; Chakravarty, Sarvajit; Perumattam, John J.; Dugar, Sundeep; Lu, Qing; Liang, Xi published a patent.Electric Literature of 256935-86-1 The title of the patent was Preparation of 5-[4-benzylpiperidinyl(piperazinyl)]-indolecarboxamides as inhibitors of p38 kinase. And the patent contained the following:

The title compounds [I; one Z2 = CA, CR8A and the other = CR1, CR12, NR6, N (wherein R1, R6, R8 = H, noninterfering substituent; A = WiCOXjY; Y = COR2, an isostere; R2 = H, noninterfering substituent; W, X = spacer of 2-6Å; i, j = 0-1); Z3 = NR7, O; R3 = noninterfering substituent; n = 0-3; L1, L2 = linker; R4 = noninterfering substituent; m = 0-4; Z1 = CR5, N (R5 = H, noninterfering substituent); l, k = 0-2, wherein the sum of l and k = 0-3; Ar = aryl substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24Å] which inhibit p38-α kinase (biol. data given), were prepared Thus, treating 6-methoxy-(4-benzylpiperidinyl)-indole-5-carboxamide with oxalyl chloride in CH2Cl2 afforded the indole-5-carboxamide II. 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 indolecarboxamide benzylpiperidinyl benzylpiperazinyl preparation p38 kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) 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 December 31, 2022, Tan, Jian-Ping; Li, Kehan; Shen, Boming; Zhuang, Cheng; Liu, Zanjiao; Xiao, Kai; Yu, Peiyuan; Yi, Bing; Ren, Xiaoyu; Wang, Tianli published an article.Safety of 1,5-Dimethyl-1H-indole-2-carbaldehyde The title of the article was Asymmetric synthesis of N-bridged [3.3.1] ring systems by phosphonium salt/Lewis acid relay catalysis. And the article contained the following:

Here, a general and modular method for constructing these pseudo-natural N-bridged [3.3.1] ring systems via cascade process by bifunctional phosphonium salt/Lewis acid relay catalysis were reported. A wide variety of substrates bearing an assortment of functional groups (59 examples) were compatible with this protocol. Other features include a [3 + 2] cyclization/ring-opening/Friedel-Crafts cascade pathway, excellent reactivities and stereoselectivities, easily available starting materials, step economy and scalability. The obtained enantioenriched products showed potential of preliminary anticancer activities. Insights gained from our studies are expected to advance general efforts towards the catalytic synthesis of challenging even unprecedented chiral PNPs, offering new opportunities for bioactive small-mol. discovery. The experimental process involved the reaction of 1,5-Dimethyl-1H-indole-2-carbaldehyde(cas: 883526-76-9).Safety of 1,5-Dimethyl-1H-indole-2-carbaldehyde

The Article related to bridged indole alkaloid preparation antitumor, Heterocyclic Compounds (One Hetero Atom): Other Areno- and Diarenopyridines (Acridines, Quinolizines, etc.) and other aspects.Safety of 1,5-Dimethyl-1H-indole-2-carbaldehyde

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 31, 2009, Luo, Ren-Shi; Weng, Jiang; Ai, Hui-Bing; Lu, Gui; Chan, Albert S. C. published an article.Application In Synthesis of H-Idc-OH The title of the article was Highly efficient asymmetric Michael reaction of aldehydes to nitroalkenes with diphenylperhydroindolinol silyl ethers as organocatalysts. And the article contained the following:

New dihydroindole and perhydroindole derivatives were synthesized in good yields and evaluated as chiral catalysts in the asym. Michael reaction of aldehydes to nitroalkenes. (2S,3aS,7aS)-Diphenylperhydroindolinol silyl ether facilitated the reaction of a wide range of aldehyde and nitroalkene substrates, providing Michael adducts in nearly optically pure form (99% ee), good yields and high diastereoselectivities (syn/anti up to 99:1). These results show that perhydroindole derivatives can be highly efficient organocatalysts for the asym. Michael reaction, exhibiting comparable or even better enantioselectivities than proline derivatives The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Application In Synthesis of H-Idc-OH

The Article related to michael stereoselective aldehyde nitroalkene silyloxydiphenylmethylindole catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Aldehydes and Derivatives, Including Sulfur Analogs and other aspects.Application In Synthesis of H-Idc-OH

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