Tag: 100-200

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 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

On June 3, 2010, Staehle, Wolfgang; Kober, Ingo; Schiemann, Kai; Schultz, Melanie; Wienke, Dirk published a patent.Category: indole-building-block The title of the patent was Preparation of benzo[b][1,6]naphthyridines as inhibitors of autotaxin for the treatment of tumors. And the patent contained the following:

Title compounds I [D = D'[R1]m; D’ = Ar, Het1; Het1 = heterocycle with provisos; R1 = H, halo, OH, etc.; R4 = [R4′]p; R4′ = H, halo, OH, etc.; m = 0-5; p = 1-4; R2, R3 = alkyl with provisos; R5 = H, halo, OH, etc.; X, Y = CH2, (CH2)2, CO, etc.; Z = O, NH, CH=CH, etc.] and their pharmaceutically acceptable salts and formulations were prepared Benzo[b][1,6]naphthyridine II is an example from the disclosed process. Title compounds I exhibited inhibition activity in autotaxin assays. 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 benzonaphthyridine preparation autotaxin inhibition antitumor agent, 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

Hsu, Shih-Fan; Ko, Chih-Wei; Wu, Yao-Ting published an article in 2011, the title of the article was Cobalt-Catalyzed Carbon-Carbon Bond Formation: Synthesis and Applications of Enantiopure Pyrrolidine Derivatives[1].Computed Properties of 79815-20-6 And the article contains the following content:

In the presence of cobalt catalysts and tetramethylethylenediamine (TMEDA), the iodine atom in (S)-2-(iodomethyl)pyrrolidines was replaced by an aryl or an alkynyl group from the corresponding Grignard reagent, and the coupling products were obtained in good to excellent yields (16 examples; 75-94% yields). The scope and limitations of this protocol were examined The stereochem. of the pyrrolidines was unaffected by the reaction conditions. The coupling products are important building blocks of phenanthroindolizidine alkaloids. Palladium-catalyzed formal [4+2] cycloaddition of 2,2′-diiodobiphenyl with the thus-generated (S)-2-(3-trimethylsilyl-2-propynyl)pyrrolidine gave a good yield of the desilylated phenanthrene, which was then converted into unnatural (+)-(S)-tylophorine by the Pictet-Spengler cyclization. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Computed Properties of 79815-20-6

The Article related to pyrrolidine enantiopure preparation cross coupling cobalt catalyzed, tylophorine synthesis cross coupling cobalt catalyzed, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Computed Properties 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 July 31, 2014, Tanimori, Shinji; Inaba, Ushio; Kato, Yoshihiro; Ura, Haruna; Kashiwagi, Hiroaki; Nishimura, Takeshi; Kirihata, Mitsunori published an article.Related Products of 65417-22-3 The title of the article was Efficient synthesis of useful heterocycles via transition metal-catalyzed cascade processes. And the article contained the following:

This paper reports our recent results from synthesis of some useful heterocycles, for example oxazolidinones, indoles, and quinoxalinones, by transition metal-catalyzed cascade processes. The scope and limitations of these procedures and the reaction mechanism for formation of the heterocycles are also discussed. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Related Products of 65417-22-3

The Article related to oxazolidinone indole quinoxalinone preparation transition metal catalyzed cascade process, Heterocyclic Compounds (More Than One Hetero Atom): General and other aspects.Related Products 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 August 31, 1979, Kaneko, Chikara; Naito, Toshihiko; Hashiba, Marimi; Fujii, Harue; Somei, Masanori published an article.HPLC of Formula: 65417-22-3 The title of the article was Studies on the N-oxides of π-deficient N-heteroaromatics. Part XXXIII. A novel synthesis of revenine and related alkaloids by means of a photo-rearrangement reaction of 4-alkoxy-2-methylquinoline 1-oxides. And the article contained the following:

Photochem. rearrangement of methylquinoline oxides I (R = Me, allyl, Me2C:CHCH2, HCCCH2) in MeOH gave quinolinones II (R1 = H, R2 = Me; R1 = Me, R2 = H) and methoxyquinolinones III. II (R = Me2C:CHCH2, R1 = Me) is the alkaloid revenine from Rutaccous plants. Chlorination of 2-methyl-4-nitroquinoline oxide by concentrated HCl gave ∼80% 4-chloro-2-methylquinoline oxide, which was treated with ROH containing KOH to give ∼80% I. Photolysis of 4-(methoxycarbonyl)-2-methylquinoline oxide in MeOH gave 25.2% Me indole-3-carboxylate, 15.7% 4-(methoxycarbonyl)-3-methylcarbostyril, 12.3% Me 1-(1,1-dimethoxyethyl)indole-3-carboxylate, 11.5% Me 2-methylindole-3-carboxylate, and 4.3% 4-(methoxycarbonyl)-1-methylcarbostyril. The mechanism of the photorearrangement was discussed. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).HPLC of Formula: 65417-22-3

The Article related to revenine, alkenyloxyquinolone, rearrangement photochem alkoxyquinoline oxide, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.HPLC of Formula: 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 October 31, 2019, Zhang, Yin-Jun; Chen, Chang-Sheng; Liu, Hao-Tian; Chen, Jia-Lin; Xia, Ying; Wu, Shi-Jin published an article.Computed Properties of 79815-20-6 The title of the article was Purification, identification and characterization of an esterase with high enantioselectivity to (S)-ethyl indoline-2-carboxylate. And the article contained the following:

Objective: To purify an esterase which can selectively hydrolyze (R,S)-Et indoline-2-carboxylate to produce (S)-indoline-2-carboxylic acid and characterize its enzymic properties. Results: An intracellular esterase from Bacillus aryabhattai B8W22 was isolated and the purified protein was identified as a carboxylesterase by MALDI-TOF mass spectrometry. The enzyme (named BaCE) was 59.03-fold purification determined to be of approx. 35 kDa. Its specific activity was 0.574 U/mL with 20% yield. The enzyme showed maximum activity at pH 8.5 and 30°C and was stable at 20-30°C using pNPB as the substrate. The esterase demonstrated high enantioselectivity toward (S)-Et indoline-2-carboxylate with 96.55% e.e.p at 44.39% conversion, corresponding to an E value of 133.45. Conclusions: In this study, a new esterase BaCE with an apparent mol. mass of 35 kDa was purified to homogeneity for the first time. The esterase from Bacillus aryabhattai B8W22 was isolated with a purification more than 59-fold and a yield of 20% by anion exchange chromatog. and hydrophobic interaction chromatog. And its biochem. characterization were described in detail with pNPB as substrate. It displayed high enantioselectivity toward (S)-Et indoline-2-carboxylate. We next plan to highly express esterase BaCE in Escherichia coli, and apply it to industrial production of (S)-indoline-2-carboxylic acid. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Computed Properties of 79815-20-6

The Article related to esterase enantioselectivity ethyl indoline 2carboxylate, (s)-indoline-2-carboxylic acid, bacillus aryabhattai b8w22, characterization, esterase, purification, Enzymes: Separation-Purification-General Characterization and other aspects.Computed Properties 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 September 5, 2014, Chen, Hui; Wang, Jiang; Zhou, Shengbin; Liu, Hong published an article.COA of Formula: C9H9NO2 The title of the article was Asymmetric Synthesis of Chiral Heterocyclic Amino Acids via the Alkylation of the Ni(II) Complex of Glycine and Alkyl Halides. And the article contained the following:

An investigation into the reactivity profile of alkyl halides led to the development of a new method for the asym. synthesis of chiral heterocyclic amino acids. This protocol involves the asym. alkylation of the Ni(II) complex of glycine, [NiL] (H2L = N-[phenyl[2-[[[(2S)-1-(phenylmethyl)-2-pyrrolidinyl]carbonyl]amino]phenyl]methylene]-glycine), to form an intermediate, which then decomposes to form valuable chiral amino acids in high yields and with excellent diastereoselectivity. The chiral amino acids underwent a smooth intramol. cyclization process to afford the valuable chiral heterocyclic amino acids in high yields and enantioselectivities. This result paves the way for the development of a new synthetic method for chiral heterocyclic amino acids. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).COA of Formula: C9H9NO2

The Article related to nickel pyrrolidinylcarbonylaminophenylmethyleneglycine complex preparation alkylation, asym preparation chiral heterocyclic amino acid, Inorganic Chemicals and Reactions: Coordination Compounds and other aspects.COA of Formula: C9H9NO2

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 10, 2012, Calderon, Felix; Vidal-Mas, Jaume; Burrows, Jeremy; de la Rosa, Juan Carlos; Jimenez-Diaz, Maria Belen; Mulet, Teresa; Prats, Sara; Solana, Jorge; Witty, Michael; Gamo, Francisco Javier; Fernandez, Esther published an article.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the article was A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. And the article contained the following:

From the 13 533 chem. structures published by GlaxoSmithKline in 2010, we identified 47 quality starting points for lead optimization. One of the most promising hits was the TCMDC-139046, a mol. presenting an indoline core, which is well-known for its anxiolytic properties by interacting with serotonin antagonist receptors 5-HT2. The inhibition of this target will complicate the clin. development of these compounds as antimalarials. Herein, we present the antimalarial profile of this series and our efforts to avoid interaction with this receptor, while maintaining a good antiparasitic potency. By using a double-divergent structure-activity relationship anal., we have obtained a novel lead compound harboring an indoline core. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

The Article related to sar antimalaria 5ht antagonist indole, tres cantos antimalarial set, divergent sar, indoline, malaria, open-innovation, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Application In Synthesis 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

Saravanan Prabhu, Nadarajan; Ayyadurai, Niraikulam; Deepankumar, Kanagavel; Chung, Taeowan; Lim, Dong Joon; Yun, Hyungdon published an article in 2012, the title of the article was Reassignment of sense codons: Designing and docking of proline analogs for Escherichia coli prolyl-tRNA synthetase to expand the genetic code.Computed Properties of 79815-20-6 And the article contains the following content:

Amino acyl-tRNA synthetases (AARSs) play a vital role in protein synthesis by catalyzing the aminoacylation of tRNA with its cognate amino acid. More recently, the endogenous AARS has been reported to recognize the close structural analogs of its cognate amino acid and helps in the in vitro and in vivo incorporation of analogs into recombinant proteins. By exploiting this substrate promiscuity, a number of non-canonical amino acids were successfully incorporated into the recombinant proteins. However, the incorporation efficiency varies with the different structural analogs depending on their reactivity towards the tRNA synthetases, which is due to the interaction and accommodation in the active site. Here, to analyze the incorporation efficiency of different proline analogs and to predict the active site residues responsible for the recognition, we carried out mol. docking study with the modeled Escherichia coli prolyl-tRNA synthetase (EcProRS). We also mapped the binding mode for the reported, virtually generated proline analogs and compared it with the reported crystal structure. The reactivity of the reported analogs was correlated with the biochem. data with respect to their interaction and orientation in the active site, which demonstrates the role of active site residues for the recognition of proline analogs and some new substrates such as chloro, bromo and iodoproline for EcProRS. We also rationally designed a EcProRS mutant for desired proline analog and validated by docking simulation with 3D model structure. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Computed Properties of 79815-20-6

The Article related to sense codon docking proline escherichia prolyl trna synthetase modeling, Enzymes: Separation-Purification-General Characterization and other aspects.Computed Properties 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