Month: November 2022

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

On December 10, 2002, Munchhof, Michael John; Sobolov-Jaynes, Susan Beth; Marx, Matthew Arnold published a patent.Related Products of 52537-00-5 The title of the patent was Preparation of thienopyrimidines and thienopyridines as anticancer agents. And the patent contained the following:

The title compounds [I and II; X1 = CH; R1 = H, alkyl, C(O)alkyl; R2 = aryl, heterocyclic; R11 = H, alkyl, C(O)NR6R9, etc.; R6 = H, alkyl, etc.; R9 = H, alkyl, etc.] and analogs useful for treating hyperproliferative disorders, were prepared E.g., a multi-step synthesis of I [X1 = N; R1 = indol-5-yl; R2 = H; R11 = Br], was given. Compounds I are effective at 0.2-2.5 g/day for a 70 kg human. 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 anticancer agent thienopyrimidine thienopyridine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products 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 January 3, 2013, Suzuki, Masaki; Kondo, Kazumi; Kurimura, Muneaki; Valluru, Krishna Reddy; Takahashi, Akira; Kuroda, Takeshi; Takahashi, Haruka; Fukushima, Tae; Miyamura, Shin; Ghosh, Indranath; Dogra, Abhishek; Harriman, Geraldine; Elder, Amy; Shimizu, Satoshi; Hodgetts, Kevin J.; Newcom, Jason S. published a patent.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Quinazolines as STEP inhibitors and their preparation and use in the treatment of central nervous system agents. And the patent contained the following:

Methods of treating disorders using quinazoline compounds of formula I that modulate STriatal-enriched tyrosine phosphatase (STEP) are described herein. Compounds of formula I wherein m is 0 and 1; L is a bond and NH and derivatives; R1 is H, C1-8 alkyl, halo, C1-8 haloalkyl, etc.; R2 is C1-8 alkoxy, benzodioxolyl, piperazinyl, halo, etc.; R3 is pyridinyl, pyrimidinyl, pyrazinyl, etc.; R4 is H, C1-8 alkyl, C1-8 alkoxy, etc.; and salts thereof, are claimed. Example compound II•3HCl was prepared by amination of 4-bromo-6-methoxy-2-(pyridin-3-yl)quinazoline with 3-aminopyridine-2-carboxamide. All the invention compounds were evaluated for their STEP inhibitory activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

The Article related to quinazoline preparation step inhibitor treatment cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 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 August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Electric Literature of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; 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 anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Electric Literature of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 1256359-96-2

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 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Application of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; 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 anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Application of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1256359-96-2

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