Month: November 2022

On June 30, 2006, Qian, Chao; Zhang, Jia-sen; Liu, Jian-qing; Li, Lu-zhen; Chen, Xin-zhi published an article.Reference of H-Idc-OH The title of the article was Study on the synthesis of S-(-)-2-Carboxyindoline. And the article contained the following:

A general synthetic route of S-(-)-2-carboxyindoline was proposed which started from o-nitrotoluene and di-Et oxalate, via condensation, nitro-group reduction, heterocyclic reduction and hydrolysis, 2-carboxyindoline was achieved with total yield of 40.6%. Especially, using 10% Pd-C as catalysts, the heterocycle is reduced easily with hydrogen at 160° and 6.2 MPa, the catalysts also can be reclaimed. Through steps of chlorination, esterification, fractional crystallization, and hydrolysis, the S-(-)-2-carboxyindoline was resolved with L-carnitine oxalate as the chiral resolution reagent. The titled product can be achieved with 32% yield and [α20589 = -27.5] (c = 1.0, DMSO). The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Reference of H-Idc-OH

The Article related to carboxyindoline preparation nitrotoluene chiral resolution carnitine oxalate, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Reference 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

Shalygina, E. E.; Kobylinskii, D. V.; Ivanovskii, S. A.; Balakin, K. V.; Dorogov, M. V.; Toporova, T. A. published an article in 2004, the title of the article was Synthesis and properties of 1-acylindolinesulfonamides.COA of Formula: C12H12ClNO3S And the article contains the following content:

Title compounds I and II were prepared by N-acylation of indoline, bromination and chlorosulfonylation (or just chlorosulfonylation), and amidation. Several properties indicative of potential pharmacol. activities were determined The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).COA of Formula: C12H12ClNO3S

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

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, 2021, Qiu, Renhua; Ou, Yifeng; Yang, Tianbao published a patent.Electric Literature of 52537-00-5 The title of the patent was Green preparation of N-(2-arylcarboxaldehyde)-1-aminoindole derivative and its application. And the patent contained the following:

The present invention relates to the green preparation of N-(2-arylcarboxaldehyde)-1-aminoindole derivative and its application. In particular, the preparation method comprises a step of reacting indoline compounds with o-nitrobenzyl alcs. as main raw materials in the presence of an acetic acid and tetraethylammonium iodide as an additive under a solvent condition, irradiated with 385-405 nm UV light at room temperature, and reacted for 24 h. to obtain N-(2-aryl formaldehyde)-1-aminoindole derivative I, II, III, IV (wherein, R1 = 2,5-di-Me, 3-Me, 4-fluoro, 5-fluoro, 5-chloro, 5-bromo, 5-iodine, 5-Me, 5-benzyloxy, 5-methoxy, 5-methylformate, 5-cyano, 5-nitro, 5,6-dichloro, 6-chloro, 7-chloro; R2 = 2-Me, 3-Me, 4-bromo, 4-(3-furan), 4-(3-thiophene), 4-(2-naphthyl), 4,5-dimethoxy, 5-Me, 5-chloro, 5-Me formate; R3 = Me, benzene, 2-naphthyl, 3-furan, 2-chlorophenyl, 3-methylphenyl, 3-benzyloxyphenyl, 4-methoxyphenyl; and R4 and R5 = 4-nitro and Ph, 4,5-methylenedioxy and phenyl). The inventive method has the advantages of low cost, high yield, simple and easy to operate, no metal and photocatalyst, green and environmental protection, has potential industrial applications and the obtained fluorescent probe has the characteristics of high efficiency and sensitivity. 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 arylcarboxaldehyde aminoindole derivative green preparation fluorescent probe, 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

On August 20, 2021, Ou, Yifeng; Yang, Tianbao; Tang, Niu; Yin, Shuang-Feng; Kambe, Nobuaki; Qiu, Renhua published an article.Formula: C8H8ClN The title of the article was Photo-Induced N-N Coupling of o-Nitrobenzyl Alcohols and Indolines To Give N-Aryl-1-amino Indoles. And the article contained the following:

A novel method to synthesize N-aryl-1-amino indoles I [R = H, Me, Ph, etc.; R1 = H, 6-Me, 5-Cl, etc.; R2 = H, 4-F, 5-Br, etc.] was established by the photoinduced N-N coupling reaction. This protocol was operated by treatment of o-nitrobenzyl alcs. and indolines in the presence of TEAI and acetic acid with a 24 W UV light-emitting diode (LED) (385-405 nm) irradiation The products bearing an aldehyde group can be further transformed to fluorescent probes based on Rhodamine derivative, which shows a high specificity and sensitivity for Fe3+. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Formula: C8H8ClN

The Article related to aryl amino indole preparation, nitrobenzyl alc indoline photo induced coupling, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C8H8ClN

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 8, 1982, there was a patent about fungicides.Category: indole-building-block The title of the patent was 1-(α-Chloroacetyl)-6-substituted indolines. And the patent contained the following:

Title indolines I [R = COCH2Cl (II), COCH2NO2] were prepared by acylating I (R = H) in the presence of bases. Thus, 14.7 g ClCH2COCl was added to a mixture of 20 g I (R = H) and 14.4 g Et3N in C6H6 with cooling and the whole stirred 30 min with cooling and 2 h at 30-40° to give 74.8% II. II showed fungicidal activity at 1000 ppm. 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 indoline chloro fungicide preparation, chloroindoline acyl fungicide 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 March 27, 2008, Chen, Li; Zhang, Jing; Zhang, Zhuming; Yang, Song published a patent.Formula: C8H8ClN The title of the patent was Oxindole derivatives as anticancer agents and their preparation, pharmaceutical compositions and use in the treatment of proliferative and oncological diseases. And the patent contained the following:

There is provided compounds of the formula I, which exhibited activity as anticancer agents. Compounds of formula I wherein X is H, halo, CN, lower alkyl, lower alkenyl, lower alkynyl, etc.; V is H and halo; Y is (un)substituted lower alkylamino, (un)substituted (hetero)arylamino, (un)substituted dialkylamino, (un)substituted lower alkoxy, (un)substituted (hetero)aryloxy, etc.; W is O, N and a single bond; n is 1 – 3; R6 is (un)substituted heteroaryl; and their pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by condensation of 6-chlorooxindole with 3-chlorobenzaldehyde; the resulting 3-(3-chlorobenzylidene)-6-chlorooxindole underwent hydride reduction to give 3-(3-chlorobenzyl)-6-chlorooxindole, which underwent bromination to give 3-bromo-3-(3-chlorobenzyl)-6-chlorooxindole, which underwent amination with 4-propoxyaniline to give compound II. All the invention compounds were evaluated for their anticancer activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Formula: C8H8ClN

The Article related to oxindole derivative preparation anticancer treatment proliferative oncol disease, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C8H8ClN

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

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 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 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