Day: November 3, 2022

On May 7, 1998, Bromidge, Steven M.; Dabbs, Steven; Davies, David T.; Duckworth, D. Malcolm; Forbes, Ian T.; Ham, Peter; Jones, Graham E.; King, Frank D.; Saunders, Damian V.; Starr, Susannah; Thewlis, Kevin M.; Wyman, Paul A.; Blaney, Frank E.; Naylor, Christopher B.; Bailey, Fiona; Blackburn, Thomas P.; Holland, Vicky; Kennett, Guy A.; Riley, Graham J.; Wood, Martyn D. published an article.Related Products of 52537-00-5 The title of the article was Novel and Selective 5-HT2C/2B Receptor Antagonists as Potential Anxiolytic Agents: Synthesis, Quantitative Structure-Activity Relationships, and Molecular Modeling of Substituted 1-(3-Pyridylcarbamoyl)indolines. And the article contained the following:

The synthesis, biol. activity, and mol. modeling of a novel series of substituted 1-(3-pyridylcarbamoyl)indolines are reported. These compounds are isosteres of the previously published indole urea SB-206553 and illustrate the use of aromatic disubstitution as a replacement for fused five-membered rings in the context of 5-HT2C/2B receptor antagonists. By targeting a region of space previously identified as sterically allowed at the 5-HT2C receptor but disallowed at the 5-HT2A receptor, a number of compounds which are the most potent and selective 5-HT2C/2B receptor antagonists yet reported, were identified. 1-(3-Pyridylcarbamoyl)-5-methylthio-6-trifluoromethylindoline was selected on the basis of its overall biol. profile for further evaluation as a novel, potential nonsedating anxiolytic agent. A CoMFA anal. of these compounds produced a model with good predictive value and in addition good qual. agreement with both a 5-HT2C receptor model and a proposed binding mode for this class of ligands within that model. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Related Products of 52537-00-5

The Article related to pyridylcarbamoylindoline preparation 5ht receptor antagonist anxiolytic, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Related Products of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On June 15, 2015, Ferencz, Zs.; Adok-Sipiczki, M.; Hannus, I.; Sipos, P.; Palinko, I. published an article.Name: H-Idc-OH The title of the article was Structural features of intercalated CaFe-layered double hydroxides studied by X-ray diffractometry, infrared spectroscopy and computations. And the article contained the following:

The intercalation of various N-containing carboxylic acid anions into CaFe-layered double hydroxides was performed by the dehydration-rehydration method. Particular attention was paid to the effect of solvent mixture used during preparation It was found that various solvent mixtures resulted in different interlayer distances and, thus, different arrangements of the anions between the layers. The dimensions of the intercalated anions and detailed anal. of the IR spectra gave clues for the reasonable prediction of the spatial arrangements of the anions in the interlamellar space. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Name: H-Idc-OH

The Article related to calcium iron layered double hydroxide intercalation, Inorganic Chemicals and Reactions: Metal-Containing Salts and Related Metal-Containing Compounds and other aspects.Name: H-Idc-OH

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽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 31, 1982, Kaneko, Chikara; Fujii, Harue; Kawai, Shinji; Hashiba, Kazuhiko; Karasawa, Yoshio; Wakai, Masue; Hayashi, Reiko; Somei, Masanori published an article.Reference of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Studies on the N-oxides of 蟺-deficient N-heteroaromatics. XXXVI. Studies on oxazepine derivatives. XII. Photochemical and thermal Michael reactions of alcohols with methyl 2-phenyl-3,1-benzoxazepine-5-carboxylate and its derivatives. And the article contained the following:

Irradiation (鈮?00 nm) of Me 2-phenyl-3,1-benzoxazepine-5-carboxylate in an alc. afforded Z-2-BzNHC6H4C(:COR)CO2Me (I, R = Me, Et, CHMe2, CMe3, allyl) as the major addition product. In contrast, thermal reaction of the oxazepine with a primary alc. in the presence of NEt3 led to the exclusive formation of E-I. Similar addition products were also obtained stereoselectively from 3,1-benzoxazepines having an acetyl group at the 5-position. E-I and Z-I were equilibrated photochem. and the stereochem. of the two isomers was determined by 1H-NMR. An explanation is proposed for the stereoselectivities observed in the photochem. and thermal reactions. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Reference of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to phenylbenzoxazepine carboxylate alcoholysis photochem thermal, benzoxazepinecarboxylate alcoholysis thermal photochem, benzamidophenylacrylate alkoxy isomer, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Esters, Acyl Peroxides, Acyl Halides and other aspects.Reference of Methyl 2-methyl-1H-indole-3-carboxylate

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽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, 2020, Shi, Zhuangzhi; Dong, Ben published a patent.Category: indole-building-block The title of the patent was Preparation method of indole compound for improving yield. And the patent contained the following:

A simple preparation method of indole compound capable of improving yield, and easy to synthesize without any addnl. reducing agent is provided. 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 indole 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聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On April 1, 1989, Muratake, Hideaki; Natsume, Mitsutaka published an article.Synthetic Route of 57817-04-6 The title of the article was Preparation of alkyl-substituted indoles in the benzene portion. Part 2. And the article contained the following:

Tosylpyrroles I (R1 = H, Me; R2 = H, Me, prenyl; R3 = alkyl, Ph, vinyl, protected CH2CH2CHO, H; Ts = tosyl) were treated with H2SO4 to give indoles II (R4 = Ts), which were converted to II (R4 = H). I were prepared from 1-tosyl-2-pyrrolecarboxaldehyde and 2-[3-(1,3-dioxolan-2-yl)propionyl]-1-tosylpyrrole. The experimental process involved the reaction of 7-Isopropyl-1H-indole(cas: 57817-04-6).Synthetic Route of 57817-04-6

The Article related to indole alkyl, alkylindole, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Synthetic Route of 57817-04-6

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽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 30, 1997, Nilsson, Kurt G. I. published a patent.SDS of cas: 130539-43-4 The title of the patent was Method of producing derivatives of β-D-glucosyl-1,4-N-acetyl-β-D-glucose. And the patent contained the following:

Disclosed is a method of producing a compound which contains the G1cβ1-4G1cN structure involving reacting ≥1 donor substance G1cβOR where R is an organic group, and ≥1 acceptor substance which is a glucopyranosamino derivative having the formula G1cNR”-R”’, wherein NR” is an azido, 2-N-acetyl-, 2-N-phthalimido, or an organic group bound to the 2-N-group of glucosamine, wherein R”’ is a glycosidically bound fluoro or is an O-, C-, N- or S-glycosidically bound aliphatic or aromatic compound, with the optional proviso that if NR” is NHAc then R”’ is not OH and if NR” is not NHAc then R”’ may be OH, in the presence of Bullera singularis or an enzyme commission (E.C.) group 3.2 glycosidase of essentially the same structure as an E.C. group 3.2 glucosidase obtained from B. singularis to form the G1cβ1-4G1cN derivative; and optionally isolating the compound which contains the G1cβ1-4G1cN structure. The experimental process involved the reaction of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside(cas: 130539-43-4).SDS of cas: 130539-43-4

The Article related to cellobiose derivative synthesis bullera glucosidase, Fermentation and Bioindustrial Chemistry: Pharmaceuticals (Including Nutrients) and other aspects.SDS of cas: 130539-43-4

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 13, 1995, Nilsson, Kurt published a patent.Application In Synthesis of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside The title of the patent was Method of producing derivatives of lactosamine. And the patent contained the following:

Disclosed is a method of producing compounds with β1-4 linkage which contains the lactosamine structure involving reacting ≥1 donor substance GalβOR where R is an organic group, and ≥1 acceptor substance which is a glucopyranosamino derivative having the formula GlcNR’-R”, wherein NR’ is an azido, 2-N-acetyl-, 2-N-phthalimido, or an organic group bound to the 2-N group of glucosamine, wherein R” is a glycosidically bound F- or is an O-, C-, N-, or S- glycosidically bound aliphatic or aromatic compound, with the proviso that if NR’ is NHAc then R” is not OH and if NR’ is not NHAc then R” may be OH, in the presence of Bullera singularis or an E.C. group 3.2 glycosidase of essentially the same structure as an E.C. group 3.2 glycosidase obtained from B. singularis to form the lactosamine derivative; and optionally isolating the compound with β1-4 linkage which contains the lactosamine structure. The experimental process involved the reaction of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside(cas: 130539-43-4).Application In Synthesis of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside

The Article related to lactosamine derivative production lactose transglycosylation galactosidase, Fermentation and Bioindustrial Chemistry: Pharmaceuticals (Including Nutrients) and other aspects.Application In Synthesis of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside

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 April 6, 2001, Blixt, Ola; Brown, Jillian; Schur, Melissa J.; Wakarchuk, Warren; Paulson, James C. published an article.Recommanded Product: 130539-43-4 The title of the article was Efficient Preparation of Natural and Synthetic Galactosides with a Recombinant β-1,4-Galactosyltransferase-/UDP-4′-Gal Epimerase Fusion Protein. And the article contained the following:

The numerous biol. roles of LacNAc-based oligosaccharides have led to an increased demand for these structures for biol. studies. In this report, an efficient route for the synthesis of β-galactosides using a bacterial β-4-galactosyltransferase/-UDP-4′-gal-epimerase fusion protein is described. The lgtB gene from Neisseria meningitidis and the galE gene from Streptococcus thermophilus were fused and cloned into an expression vector pCW. The fusion protein transfers galactose to a variety of different glucose- and glucosamine-containing acceptors, and utilizes either UDP-galactose or UDP-glucose as donor substrates. A crude lysate from Escherichia coli expressing the fusion protein is demonstrated to be sufficient for the efficient preparation of galactosylated oligosaccharides from inexpensive UDP-glucose in a multigram scale. Lysates containing the fusion protein are also found to be useful in the production of more complex oligosaccharides in coupled reaction mixtures , e.g., in the preparation of sialosides from N-acetylglucosamine. Thus, bacterially expressed fusion protein is well suited for the facile and economic preparation of natural oligosaccharides and synthetic derivatives based on the lactosamine core. The experimental process involved the reaction of Ethyl 2-deoxy-2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-thio-beta-D-glucopyranoside(cas: 130539-43-4).Recommanded Product: 130539-43-4

The Article related to oligogalactoside preparation escherichia recombinant fusion protein, dna sequence gale gene, Fermentation and Bioindustrial Chemistry: Pharmaceuticals (Including Nutrients) and other aspects.Recommanded Product: 130539-43-4

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 April 7, 2022, Borjesson, Ulf; Perry, Matthew William Dampier; Grebner, Christoph; Michaelides, Iacovos Neal; Hayhow, Thomas George Christopher; Kettle, Jason Grant; Collie, Gavin William; Storer, Robert Ian; Bagal, Sharanjeet Kaur; Fallan, Charlene published a patent.Recommanded Product: Methyl 2-(6-bromo-1H-indol-3-yl)acetate The title of the patent was Synthesis of heterocyclic substituted pyrimidine anticancer agents. And the patent contained the following:

The synthesis of heterocyclic substituted pyrimidine anticancer agents I, wherein A is a protein binder unit; Z can be a bicyclic heterocyclic ring system with multiple heteroaroms N, O, S; Y can be a pyrimidine dione moiety; R can be a substituent on any available C or N such that alkyl, alkenyl, alkynyl or related groups with optional halo, nitrile, amino or similar groups; L, as a linker, can be an (un)saturated framework comprising C and H atoms and at least one heteroatom; and n can be an integer between 0-3 are prepared as pharmaceutically acceptable salts. Of note, II demonstrated a Cereblon HTRF IC50 binding of 2.1μM and can be employed in the treatment of cancers in humans or animals such that solid tumors, BRD4-sensitive tumors. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Recommanded Product: Methyl 2-(6-bromo-1H-indol-3-yl)acetate

The Article related to heterocyclic pyrimidine anticancer preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 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 May 28, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Category: indole-building-block The title of the patent was Preparation of as 2-oxoindoles CGRP receptor antagonists. And the patent contained the following:

Title compounds I [R1 = 2-oxoindole with provisos; R2 = H, alkyl; R3 = H, alkylene, etc.; R4 = H, alkylene, etc.; U = N, N-oxide, CR5; V = N, N-oxide, CR6; X = N, N-oxide, CR7; Y = N, CR6; R5 = H, hyalo, CN, etc.; R6 = H, alkyl, etc.; R7 = H, halo, CN. etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, coupling of chloropyrimide II and amine III afforded claimed oxoindole IV. In CGRP receptor antagonists assays, 4-examples of compounds I exhibited Ki values ranging from 15-535 nM. 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 oxoindole preparation cgrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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