Category: indole-building-block

On December 18, 2012, Bunescu, Ala; Wang, Qian; Zhu, Jieping published an article.SDS of cas: 65417-22-3 The title of the article was Synthesis of indoles by copper-catalyzed heteroannulation of o-aminophenylboronic acid pinacol esters with β-keto esters. And the article contained the following:

Copper-catalyzed coupling of o-aminophenylboronic acid pinacol esters with β-keto esters afforded, under mild base-free oxidative conditions, 2,3-disubstituted indoles featuring a key Chan-Lam-type carbon-carbon bond-forming reaction. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).SDS of cas: 65417-22-3

The Article related to indole preparation, aminophenylboronic acid pinacol ester keto ester copper catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.SDS of cas: 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 March 15, 2014, Luo, Ren-shi; Xie, Ling; Liao, Jian-hua; Zhang, Jian published an article.Product Details of 79815-20-6 The title of the article was Synthesis and characterization of novel indole chiral amino alcohols. And the article contained the following:

With (S)-indole-2-carboxylic acid and (S)-octahydroindole-2-carboxylic acid as raw material, processed by esterification, protection, Grignard reaction and reduction by Pd/C, two new chiral indole derivative (S)-(2-octahydroindole) di-Ph methanol and (S)-(2-indolinyl)-diphenyl methanol were synthesized in high yield. The total yields were resp. 88.3% and 83.7%, the structure of the products were characterized by 1HNMR, 13CNMR and HRMS spectra. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Product Details of 79815-20-6

The Article related to synthesis characterization indole chiral amino alc esterification grignard reduction, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Product Details 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 March 15, 2005, Mavunkel, Babu J.; Chakravarty, Sarvajit; Perumattam, John J.; Dugar, Sundeep; Lu, Qing; Liang, Xi published a patent.Recommanded Product: 256935-86-1 The title of the patent was Preparation of indolylcarboxamide derivatives as inhibitors of p38 kinase. And the patent contained the following:

Title compounds I [X independently = CA, CR4A, CR5, CR52, NR6, or N; L1 = CO, SO2, or alkylene; L2 = (un)substituted-alkylene or -alkenylene; Ar = (un)substituted aryl group with substituents consisting of alkyl, alkenyl, halo, CN, etc.; Z = N or CR7 wherein R7 = H or non-interfering substituent; R1 = H, alkyl, alkenyl, alkynyl, aryl, arylalkyl, etc.; R2 independently = halo, alkyl, OH, alkoxy, etc.; R3 independently = CN, CF3, NO2, alkyl, aryl, acyl, etc.; R4 = H, halo, alkyl or alkenyl; R5 independently = H, halo, alkyl, OH, etc.; R6 = H, alkyl, alkenyl, aryl, acyl, aroyl, etc.; A = -WiCOXjY wherein Y is COR8 wherein R8 = H, (un)substituted-alkyl, -alkenyl, -alkynyl, etc.; W and X = (un)substituted-alkylene, -alkenylene, -alkynylene; Y = tetrazole, 1,2,3-triazole, 1,2,4-triazole, or imidazole and each of i and j independently = 0 or 1; m = 0-4; n = 0-3], and their pharmaceutically acceptable salts are prepared and disclosed as useful for treatment of rheumatoid arthritis. Thus, e.g., II, was prepared by carbonylation of 6-methoxy-(4-benzylpiperidinyl)-indole-5-carboxamide with oxalyl chloride and subsequent amination using 4-methylpiperazine. ELISA assays for evaluation of inhibition of p38 kinase by I revealed that all compounds of the invention possessed IC50 values in the range of 0.1-1.5 μM. I as inhibitors of p38 kinase should prove useful in the treatment of rheumatoid arthritis. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Recommanded Product: 256935-86-1

The Article related to indolylcarboxamide derivative preparation p38 kinase inhibitor antirheumatic agent, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 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 July 31, 2018, Bodunov, Vladimir A.; Galenko, Ekaterina E.; Galenko, Alexey V.; Novikov, Mikhail S.; Khlebnikov, Alexander F. published an article.Formula: C11H11NO2 The title of the article was Synthesis of substituted indole-3-carboxylates by iron(II)-catalyzed domino isomerization of 3-alkyl/aryl-4-aryl-5-methoxyisoxazoles. And the article contained the following:

The iron(II)-catalyzed domino isomerization of 3-alkyl/aryl-4-arylisoxazoles provided a selective access to a wide range of structurally diverse highly substituted indole-3-carboxylates such as I [R = H, 6-Me, 4-MeO, etc.; R1 = Me, 4-ClC6H4, 2-naphthyl, etc.; R2 = Me, pyrrolidin-1-yl]. The operational simplicity, high atom efficiency and the use of stable starting materials and an inexpensive and low-toxicity catalyst were some of the attractive features of this tandem double ring-opening-ring-closure strategy. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Formula: C11H11NO2

The Article related to indole carboxylate green preparation, isoxazole tandem isomerization iron catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.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

On February 6, 2015, Park, Jihye; Mishra, Neeraj Kumar; Sharma, Satyasheel; Han, Sangil; Shin, Youngmi; Jeong, Taejoo; Oh, Joa Sub; Kwak, Jong Hwan; Jung, Young Hoon; Kim, In Su published an article.Recommanded Product: 52537-00-5 The title of the article was Mild Rh(III)-Catalyzed C7-Allylation of Indolines with Allylic Carbonates. And the article contained the following:

The rhodium(III)-catalyzed direct allylation of indolines with allylic carbonates at room temperature is described. These transformations provide the facile and efficient construction of C7-allylated indolic scaffold I [R = Me, t-Bu, NMe2, etc; R1 = H, Me, Ph, etc.]. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 52537-00-5

The Article related to indoline allylic carbonate allylation rhodium catalyst, allylindoline preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 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

Lv, Honggui; Shi, Jingjing; Wu, Bo; Guo, Yujuan; Huang, Junjun; Yi, Wei published an article in 2017, the title of the article was One-pot synthesis of 2,3-difunctionalized indoles via Rh(III)-catalyzed carbenoid insertion C-H activation/cyclization.Recommanded Product: 65417-22-3 And the article contains the following content:

The first Rh(III)-catalyzed carbenoid insertion C-H activation/cyclization of N-arylureas R1NHC(O)R (R = N(CH3)2, NHCH3; R1 = naphth-1-yl, 2-CH3C6H4, 3-ClC6H4, 4-CH3(O)CC6H4, etc.) and α-diazo β-keto esters R2C(O)C(=N2)C(O)R3 [R2 = H, Me, Ph, CH2OCH3, CH2CH3; R3 = C(O)OCH2CH3, C(O)OCH2C6H5, ((OCH3)2)P(O), etc.] was reported. The redox-neutral reaction has the following features: good to excellent yields, broad substrate/functional group tolerance, exclusive regioselectivity, and no need for addnl. oxidants or additives, which render this methodol. as a more efficient and versatile alternative to the existing methods for the synthesis of 2,3-difunctionalized indoles e.g., I. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Recommanded Product: 65417-22-3

The Article related to indole preparation green chem regioselective, arylurea diazo keto ester bond activation cyclization rhodium catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 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

Chen, Cong; Jiao, Hongjian; Chen, Di; Tang, Tao; Xu, Ze-Feng; Duan, Shengguo; Li, Chuan-Ying published an article in 2022, the title of the article was Access to tetrahydrocarbazoles and pyrrolo[3,4-b]carbazoles through sequential reactions of triazoles and indoles.Application In Synthesis of 1,5-Dimethyl-1H-indole-2-carbaldehyde And the article contains the following content:

Tetrahydrocarbazoles I (R = H, Me; R1 = H, OMe, F, Cl, etc.; R2 = H, Me; R3 = H, Me; R4 = Me, allyl; R5 = Et, t-Bu; R6 = Me, Ts, benzenesulfonyl, etc.; R7 = Ac, Boc, Bz, etc.) and pyrrolo[3,4-b]carbazoles II could be synthesized conveniently through sequential reactions of ester-tethered 1-sulfonyl-1,2,3-triazoles III and indoles IV. The reaction conditions were mild and the procedures were quite simple. Moreover, the key intermediate α,β-unsaturated imine acted as a [2C] synthon in the [4 + 2] cycloaddition reaction, and the imino group could be used as a nucleophile to construct the fourth ring. The experimental process involved the reaction of 1,5-Dimethyl-1H-indole-2-carbaldehyde(cas: 883526-76-9).Application In Synthesis of 1,5-Dimethyl-1H-indole-2-carbaldehyde

The Article related to tetrahydrocarbazole preparation, pyrrolocarbazole preparation, indole ester sulfonyl triazole diels alder reaction, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application In Synthesis 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 1, 2021, Faltracco, Matteo; Damian, Matteo; Ruijter, Eelco published an article.Category: indole-building-block The title of the article was Synthesis of Carbazoles and Dihydrocarbazoles by a Divergent Cascade Reaction of Donor-Acceptor Cyclopropanes. And the article contained the following:

An alkylation/olefination cascade of indolecarboxaldehydes and phosphonate-functionalized donor-acceptor cyclopropanes affords functionalized dihydrocarbazoles and cyclohepta[cd]indoles in formal [3 + 3] and [4 + 3]-cycloadditions A minor modification to the reaction conditions also allowed access to the fully aromatic heterocyclic scaffolds by thermal loss of an electron-rich aryl moiety. The experimental process involved the reaction of 1,5-Dimethyl-1H-indole-2-carbaldehyde(cas: 883526-76-9).Category: indole-building-block

The Article related to indolecarboxaldehyde cyclopropane scandium catalyst tandem cycloaddition, carbazole dihydrocarbazole preparation, 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 January 1, 2008, Sayago, Francisco J.; Isabel Calaza, M.; Jimenez, Ana I.; Cativiela, Carlos published an article.Application In Synthesis of H-Idc-OH The title of the article was Versatile methodology for the synthesis and α-functionalization of (2R,3aS,7aS)-octahydroindole-2-carboxylic acid. And the article contained the following:

An improved strategy for the effective synthesis of enantiomerically pure (2R,3aS,7aS)-octahydroindole-2-carboxylic acid, based on the formation of a trichloromethyloxazolidinone derivative, has been developed. Addnl., the completely diastereoselective α-alkylation of such oxazolidinone provides a very convenient and concise route to enantiopure α-tetrasubstituted derivatives of this stereoisomer of octahydroindole-2-carboxylic acid. 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 indolecarboxylic octahydro alkylated asym synthesis, indolooxazolidinone preparation stereoselective alkylation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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 May 31, 2007, Kerns, Jeffrey K.; Busch-Petersen, Jakob; Li, Huijie; Boehm, Jeffrey Charles; Nie, Hong; Taggart, John J. published a patent.Application of 860624-88-0 The title of the patent was Preparation of indolecarboxamide derivatives as inhibitors of kinase activity. And the patent contained the following:

The title compounds with general formula I [wherein X = O, S, S(O), S(O)2, etc,; R1 = H, (un)substituted alkyl, haloalkyl, heterocycloalkyl, etc.; R2 = (un)substituted alkyl, aryl, cycloalkyl, etc.; R3 = independently OH, oxo, alkyl, or haloalkyl; m = 1-3] or pharmaceutically acceptable salts thereof were prepared for the treatment of disorders associated with inappropriate IKK2 activities. In particular, I can be used for the treatment and prevention of inflammatory and tissue repair disorders, including rheumatoid arthritis, asthma, and COPD. For example, compound II was prepared in a multi-step synthesis. II exhibited IKK2 inhibitory activity with pIC50 value of 4.6 in IKK2 assay. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).Application of 860624-88-0

The Article related to preparation indolecarboxamide inhibitor kinase activity, treatment inflammatory tissue repair disorder human, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 860624-88-0

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