Day: November 8, 2022

On October 31, 2005, Segraves, Nathaniel L.; Crews, Phillip published an article.COA of Formula: C11H10BrNO2 The title of the article was Investigation of brominated tryptophan alkaloids from two Thorectidae sponges: Thorectandra and Smenospongia. And the article contained the following:

Chem. investigation of an NCI-DTP collection of Thorectandra sp. and a UCSC collection of Smenospongia sp. yielded six new brominated tryptophan derivatives : 6-bromo-1′-hydroxy-1′,8-dihydroaplysinopsin (e.g. IV), 6-bromo-1′-methoxy-1′,8-dihydroaplysinopsin (V), 6-bromo-1′-ethoxy-1′,8-dihydroaplysinopsin (VI), (-)-5-bromo-N,N-dimethyltryptophan (VII), (+)-5-bromohypaphorine (VIII), and 6-bromo-1H-indole-3-carboxylic acid Me ester (XI). Addnl., the known compounds aplysinopsin (I), 1′,8-dihydroaplysinopsin (II), 6-bromo-1′,8-dihydroaplysinopsin (III), (1H-indole-3-yl)acetic acid (IX), and (6-bromo-1H-indol-3-yl)acetic acid Me ester (X) were also encountered. The structures of IV-VIII and XI were confirmed on the basis of anal. of 1H and 13C (1D and 2D) NMR data as well as comparison to known compounds Compounds I, III-VIII, X, and XI were found to inhibit the growth of Staphylococcus epidermidis with either weak or moderate MICs. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).COA of Formula: C11H10BrNO2

The Article related to brominated tryptophan alkaloid thorectandra smenospongia antibacterial, Nonmammalian Biochemistry: Composition and Products and other aspects.COA of Formula: C11H10BrNO2

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, 2014, Heeres, Andre; Grol, Cornelius Joannes; Borst, Marcus Leonardus Gerardus; Willigers – Hogg, Sandra published a patent.Quality Control of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Substituted 3-heteroaryloxy-3-(hetero)aryl-propylamines as serotonin transporter and serotonin 5HT2C receptor modulators and their preparation. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutically acceptable salts, hydrates and solvates thereof, that have serotonin (5-HT) transporter inhibitory effects and 5-HT2C receptor antagonist or inverse agonist effects. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of using them for application in the prophylaxis or treatment of CNS disorders. Compounds of formula I wherein R1 is C6-24 aryl and C4-24 heteroaryl; R2 and R3 are independently H and C1-12 alkyl; R2R3 taken together to form (un)substituted C2-4 alkylene and heterocyclyl; R4 is (un)substituted C1-5 alkylene; W1 is (un)substituted methylene; NH and derivatives, O and S; R5, R6, R7 and R8 are independently absent, H, halo and C1-12 alkyl; U, X, Y and Z are independently C and N; E is CH, C-C1-6 alkyl, N, NH and derivatives, etc.; dashed bond is single and double bond; L and M are independently (un)substituted methylene, CH, C-C1-6 alkyl, etc.; R10, R11, R12 and R13 are independently H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, etc.; and pharmaceutically acceptable salts, hydrates and solvates thereof, are claimed. The invention compounds were evaluated for their serotonin transporter and serotonin HT2C receptor modulatory activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Quality Control of 6-Chloro-2,3-dihydro-1H-indole

The Article related to heteroaryloxypropylamine preparation serotonin transporter 5ht2c receptor modulator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Quality Control 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

Le, Truong-Giang; Pham, Hoai-Thu; Martin, James P.; Chataigner, Isabelle; Renaud, Jean-Luc published an article in 2020, the title of the article was Organocatalyzed regioselective and enantioselective synthesis of 1,4- and 1,2-dihydropyridines.Electric Literature of 79815-20-6 And the article contains the following content:

Herein, the first examples of asym. organocatalyzed synthesis of 1,2-dihydropyridines, affording enantioselective access to and partially solving regioselectivity challenges in the synthesis of dihydropyridines is reported. It has been demonstrated that through modification of organocatalysts both 1,2- and 1,4-dihydropyridines (1,2- and 1,4-DHPs) can be obtained with high regioselectivity (ratio of 1,2-DHP/1,4-DHP from 95/5 to 0/100) and enantioselectivity (33% ee for 1,2-DHPs and up to 98% ee for 1,4-DHPs) in good yields (up to 87%). The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Electric Literature of 79815-20-6

The Article related to dihydropyridine preparation green chem regioselective enantioselective organocatalyst, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature 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 February 1, 2010, Mavunkel, Babu J.; Perumattam, John J.; Tan, Xuefei; Luedtke, Gregory R.; Lu, Qing; Lim, Don; Kizer, Darin; Dugar, Sundeep; Chakravarty, Sarvajit; Xu, Yong-jin; Jung, Joon; Liclican, Albert; Levy, Daniel E.; Tabora, Jocelyn published an article.HPLC of Formula: 256935-86-1 The title of the article was Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors. And the article contained the following:

The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these compounds showed low-nanomolar activities in p38α enzymic and cell-based cytokine TNFα production inhibition assays. The optimal linkers between the piperidine and the oxalyl amide were found to be [6,5] fused ring heterocycles. Substituted indoles and azaindoles were favored structural motifs in the cellular assay. 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 piperidine based heterocyclic oxalyl amide preparation antiinflammatory, p38alpha map kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines 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 August 15, 2013, Albrecht, Brian K.; Audia, James Edmund; Cook, Andrew S.; Dakin, Les A.; Duplessis, Martin; Gehling, Victor S.; Harmange, Jean-Christophe; Naveschuk, Christopher G.; Vaswani, Rishi G. published a patent.Synthetic Route of 65417-22-3 The title of the patent was Preparation of heteroaryl amides as modulators of methyl modifying enzymes. And the patent contained the following:

The title compounds I [Z = CR2 or N; X1, X2 = N, CR3; X3 = N, CR6; no more than one of X1-X3 = N; R1, R2 = H, halo, OH, CN, etc.; or R1 and R2 are taken together with atoms to which they are bound to form (hetero)aryl, heterocyclyl, cycloalkyl; R3, R6 = H, halo, CN, etc.; or two R3 are taken together with atoms to which they are bound to form (hetero)aryl, heterocyclyl, cycloalkyl; R = (hetero)aryl, heterocyclyl, cycloalkyl, etc.], useful as agents for modulating Me modifying enzymes, were prepared Thus, reacting 3-(aminomethyl)-4,6-dimethylpyridin-2(1H)-one with 5-methyl-1-phenyl-1H-pyrazole-4-carboxylic acid afforded 26% II. Exemplified compounds I were tested against EZH2 and Y641N EZH2 mutant enzymes (data given for representative compounds I). Pharmaceutical composition comprising I is disclosed. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Synthetic Route of 65417-22-3

The Article related to heteroaryl amide preparation methyl modifying enzyme modulator antitumor, mutant ezh2 protein cancer treatment heteroaryl amide preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Synthetic Route 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 December 23, 2009, Kamikubo, Takashi; Miura, Masanori; Okuda, Takao; Maki, Keisuke; Hirayama, Fukushi; Moritomo, Ayako; Komiya, Yuriko; Matsuura, Keisuke; Ibuka, Ryotaro published a patent.SDS of cas: 52537-00-5 The title of the patent was Preparation of 2-pyridone derivatives as EP4 receptor agonists for treatment of peripheral arterial disease. And the patent contained the following:

The title compounds I [wherein L1 and L2 = independently alkylene, alkenylene, etc.; R1 = substituted aryl or heteroaryl; R2 = (un)substituted alkylamino, heteroarylamino, etc.; R3 – R5 = independently H, halo, CN, alkyl, etc.] or pharmaceutically acceptable salts thereof are prepared as prostanoid receptors type EP4 (EP4) inhibitors for the treatment of peripheral arterial disease. For example, the compound II was prepared in a multi-step synthesis. II inhibited EP4 receptor with IC50 value of 0.52 nM in rat. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).SDS of cas: 52537-00-5

The Article related to pyridone preparation prostanoid receptor agonist treatment peripheral arterial disease, prostanoid receptor ep4 agonist preparation pyridone, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.SDS of cas: 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 May 8, 2014, Tanaka, Tadashi; Konishi, Yoshitake; Kubo, Daisuke; Fujino, Masataka; Doi, Issei; Nakagawa, Daisuke; Murakami, Tatsuya; Yamakawa, Takayuki published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of (hetero)arylamines having keratinocyte proliferation inhibitory activity. And the patent contained the following:

A novel amine derivative expressed by general formula (I) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents -COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation. Thus, heteroarylamines, prepared by several steps, inhibited the proliferation of human neonatal epidermal keratinocytes and TNFα formation in LPS-stimulated Raw264.7 cells. The compounds also inhibited TPA-induced ear thickening in mice. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to heteroarylamine preparation keratinocyte proliferation tnfalpha inhibitor, tumor necrosis factor alpha inhibitor heteroarylamine preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 6-Fluoro-5-nitro-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

Jiang, Hua-Jie; Zhong, Xiu-Mei; Yu, Jie; Zhang, Ying; Zhang, Xinhao; Wu, Yun-Dong; Gong, Liu-Zhu published an article in 2019, the title of the article was Assembling a Hybrid Pd Catalyst from a Chiral Anionic CoIII Complex and Ligand for Asymmetric C(sp3)-H Functionalization.HPLC of Formula: 52537-00-5 And the article contains the following content:

An unusual hybrid palladium catalyst containing an anionic chiral CoIII complex and a chiral phosphoramidite ligand shows a high capacity for catalyzing asym. thioamide-directed C(sp3)-H arylation and delivers excellent yield and enantioselectivity (up to 99% yield, 99% ee). Significant synergy between the chiral ligand and the anion in terms of stereochem. control was observed Mechanistic studies revealed both the nature of the C-H activation and the origin of the enantioselectivity. 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 palladium catalyst chiral ligand asym functionalization arylation, c−h functionalization, chiral phosphoramidites, cobalt, palladium, synergistic effects, Heterocyclic Compounds (One Hetero Atom): Pyridines 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

On August 18, 2016, Albrecht, Brian K.; Gehling, Victor C.; Harmange, Jean-Christophe; Vaswani, Rishi G. published a patent.Category: indole-building-block The title of the patent was Preparation of substituted indolecarboxamides as modulators of methyl modifying enzymes. And the patent contained the following:

The title compounds I [R1 = alkyl, alkoxy, or OCHF2; R2 = H, Me, Et, thiazolyl, etc.; R3, R31, R4, R41 = H, CF3, Me, Et, etc. (provided that at least one of R3, R31, R4 and R41 is not H); or R3 and R4 or R31 and R41 are taken together form a Ph or cyclohexyl ring], useful for treating a variety of diseases, disorders or conditions associated with Me modifying enzymes, notably EZH1 and EZH2, were prepared E.g., a multi-step synthesis of II, starting from Me 2-methyl-1-[1-(1-methyl-2-oxopiperidin-4- yl)ethyl]-1H-indole-3-carboxylate, was described. Exemplified compounds I were tested for their EZH2 activity (data given). Also provided are pharmaceutical compositions comprising compounds I, pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with Me modifying enzymes, such as cancer. 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 indolecarboxamide pyridinylmethyl preparation modulator methyl modifying enzyme ezh1 ezh2, antitumor indolecarboxamide pyridinylmethyl preparation ezh1 ezh2 modulator, Heterocyclic Compounds (One Hetero Atom): Pyridines 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