Tag: 100-200

Deb, Indubhusan; Coiro, Daniel J.; Seidel, Daniel published an article in 2011, the title of the article was Decarboxylative formation of N-alkyl pyrroles from 4-hydroxyproline.HPLC of Formula: 79815-20-6 And the article contains the following content:

N-Alkyl pyrroles are obtained in a single step from trans-4-hydroxyproline and aldehydes or ketones in just 15 min under microwave irradiation E.g., benzoic acid-catalyzed reaction of trans-4-hydroxyproline and 4-ClC6H4CHO gave 73% N-alkyl pyrrole I. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).HPLC of Formula: 79815-20-6

The Article related to hydroxyproline reaction aldehyde ketone, alkyl pyrrole decarboxylative preparation, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.HPLC of Formula: 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

Sekhar, Abinitha S.; Saranya, T. S.; Baskar, Vaishnav; Manakadan, Asha Ashokan published an article in 2016, the title of the article was In silico approach of apoptosis induing ability of different indole derivatives by interaction with caspase9.Related Products of 256935-86-1 And the article contains the following content:

Indole compounds are well known for their wide variety of pharmacol. activities. It is the combination of benzene with pyrrole ring. Compounds having indole group are biol. important. They are used as antimicrobial, antiviral, antitubercular, antiinflammatory, anticancer, ant-diabetic and anticonvulsant agents. Because of the wide variety of biol. application, several substituted indole derivatives are studied for their mol. structure, mol. docking and bioavailability. The purpose of the study is to carry out the docking studies of indole derivatives containing electrophilic substitution and nucleophilic substitution with the anticancer target casp9. Fifty compounds were designed and by using Argus lab version 4.0.1. Their docking score was calculated and compared with the standard drug casodex. The drug likeness of compounds was performed using Lipinski rule of five. Result showed that 1,1′-(1H-indole-5,6-diyl)diethanone and 5-(trichloromethyl)-1H-indole and the phytoconstituent curcumin showed better docking score than that of the standard drug casodex. It is concluded that certain indole derivatives show greater affinity with casp9 protein. These compounds may be helpful in studying anticancer targets for casp9 protein. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Related Products of 256935-86-1

The Article related to indole derivative induce apoptosis ability anticancer target caspase protein, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Related Products of 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 June 18, 2002, Hester, Jackson B.; Rogers, Bruce N.; Jacobsen, Eric Jon; Ennis, Michael D.; Acker, Brad A.; Vander Velde, Susan L.; Frank, Kristine E. published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of tetracyclic azepinoindoles as 5-HT receptor ligands for treatment of CNS disorders. And the patent contained the following:

Title compounds I [wherein R1 = independently OH, NO2, halo, CN CF3, CF3O, or (un)substituted alkyl, alkoxy, alkanoyl(oxy), alkoxycarbonyl, (hetero)aryl, sulfamoyl, amino, carbamoyl, or SOmRe; R2 = H, alkyl, alkanoyl, aryl(carbonyl), arylalkyl, alkoxycarbonyl, aryloxycarbonyl, arylsulfonyl, or arylalkoxycarbonyl; X and Y together = (un)substituted 2-3 membered saturated or partially unsaturated chain comprising 1 or more C’s and 1 O, S, SO, SO2, or NRf; m = independently 0-2; n = 0-3; Re = independently H, alkyl, (hetero)aryl, or (hetero)arylalkyl; Rf = H, alkyl, (hetero)aryl, (hetero)arylalkyl, or is a bond to a 2-4 membered alkylene chain that forms a ring fused to the ring comprising X and Y; with provisos; or a pharmaceutically acceptable salt thereof] were prepared as serotonin 5-HT receptor ligands. For example, a neat reaction between 1,2,3,4-tetrahydroquinoline and isoamylnitrile, followed by reduction of the N-nitroso intermediate with LiAlH4, afforded 3,4-dihydro-1(2H)-quinolinylamine•HCl. Cycloaddition with benzyl 4-oxo-1-azepanecarboxylate and deprotection using Pd/C gave the desired azepinopyrroloquinoline II•HCl. The latter exhibited binding to the 5HT2c receptor with Ki of 13 nM. I are useful for the treatment of central nervous system disorders, such as anxiety, obesity, depression, schizophrenia, stress related diseases, panic disorder, a phobia, obsessive compulsive disorder, post-traumatic stress syndrome, immune system depression, a stress induced problem with the gastrointestinal or cardiovascular system, or sexual dysfunction (no data). 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 cns agent azepinopyrroloquinoline preparation, azepinoindole tetracyclic preparation serotonin receptor ligand, Heterocyclic Compounds (One Hetero Atom): Higher-Membered Rings 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

On April 30, 2012, Sikorska, Emilia; Sobolewski, Dariusz; Kwiatkowska, Anna published an article.Recommanded Product: H-Idc-OH The title of the article was Conformational preferences of proline derivatives incorporated into vasopressin analogues: NMR and molecular modelling studies. And the article contained the following:

In this study, arginine vasopressin analogs modified with proline derivatives – indoline-2-carboxylic acid (Ica), (2S,4R)-4-(naphthalene-2-ylmethyl)pyrrolidine-2-carboxylic acid (Nmp), (2S,4S)-4-aminopyroglutamic acid (APy) and (2R,4S)-4-aminopyroglutamic acid, (Apy) – were examined using NMR spectroscopy and mol. modeling methods. The results have shown that Ica is involved in the formation of the cis peptide bond. Moreover, it reduces to a great extent the conformational flexibility of the peptide. In turn, incorporation of (2S,4R)-Nmp stabilizes the backbone conformation, which is heavily influenced by the pyrrolidine ring. However, the aromatic part of the Nmp side chain exhibits a high degree of conformational freedom. With analogs [(2S,4S)-4-aminopyroglutamic acid2-3]AVP and [(2R,4S)-4-aminopyroglutamic acid2-3]AVP, introduction of the 4-aminopyroglutamic acid reduces locally conformational space of the peptides, but it also results in weaker interactions with the dodecylphosphocholine/SDS micelle. Admittedly, both analogs are adsorbed on the micelle’s surface but they do not penetrate into its core. With analog [(2R,4S)-4-aminopyroglutamic acid2-3]AVP, the interactions between the peptide and the micelle seem to be so weak that conformational equilibrium is established between different bound states. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Recommanded Product: H-Idc-OH

The Article related to arginine vasopressin proline derivative nmr mol modeling conformation preference, Mammalian Hormones: Structure and Structure-Activity Relations and other aspects.Recommanded Product: 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

On November 5, 2015, Okano, Tsubasa; Suzuki, Shinya published a patent.Product Details of 52537-00-5 The title of the patent was Preparation of imidazoline derivatives as selective adrenaline α1A receptor full agonists. And the patent contained the following:

Disclosed are compounds I [A = Q1, Q2 or Q3; R = halo; n = 1-4; or pharmaceutically acceptable salts thereof]. For example, II·2HCl was prepared via reaction of 5-chloroindolin-2-one with TMEDA/n-BuLi/1,2-dibromoethane, reduction, cyanomethylation with bromoacetonitrile, treatment with ethylenediamine/P2S5 and salt-formation. In adrenaline receptor α1 agonist activity test, the exemplified compound II·2HCl showed EC50 values (nmol/L) of 2.60 and >10000 for α1A and α1L, resp. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Product Details of 52537-00-5

The Article related to imidazoline preparation selective adrenaline alpha 1a receptor full agonist, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details 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 March 7, 2019, Goergler, Annick; Norcross, Roger; Dey, Fabian; Kusznir, Eric Andre published a patent.COA of Formula: C8H8ClN The title of the patent was Dihydrobenzimidazolones as anticancer agents and their preparation. And the patent contained the following:

The invention provides compounds of formula I which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Compounds of formula I are thus useful for the treatment of various cancers. Compounds of formula I wherein X1 and X2 are independently H, and C1-6 alkyl; W1, W2 and W3 are independently CH and N, provided that if one of W1 – W3 is N, then the other two are CH; Z is absent, (CH2)1-3, (CH2)0-2O(CH2)0-2, etc.; A is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted heterocyclyl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-fluoro-N-methyl-3-nitrobenzamide with 5-amino-1H-benzo[d]imidazol-2(3H)-one; the resulting N-methyl-3-nitro-4-((2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)amino)benzamide underwent hydrogenation to give compound II. The invention compounds were evaluated for their CRBN binding affinity. From the assay, it was determined that compound II exhibited Kd value of 0.587 μM. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).COA of Formula: C8H8ClN

The Article related to dihydrobenzimidazolone preparation anticancer crbn protein degradation, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of 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 June 19, 2020, Karjee, Pallab; Sarkar, Tanumay; Kar, Subhradeep; Punniyamurthy, Tharmalingam published an article.Application of 52537-00-5 The title of the article was Transition-Metal-Free Stereospecific Oxidative Annulative Coupling of Indolines with Aziridines. And the article contained the following:

Tandem C-N bond formation for the oxidative annulation of indolines with aziridines is accomplished employing the combination of DDQ and NaOCl at ambient conditions. Optically active aziridine can be coupled with high enantiomeric purity (>99% ee). The substrate scope, stereocontrol with the enantioenriched substrate, and scale-up are the important practical advantages. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to stereospecific oxidative annulative coupling indoline aziridine, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application 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 December 31, 2019, Li, Jie; Yao, Jiaqi; He, Weiping; Yang, Fan; Liu, Xiaoming published an article.Safety of H-Idc-OH The title of the article was Modular Synthesis of New Bicyclic Carbene Precursors. And the article contained the following:

A series of new N-heterocyclic carbene (NHC) precursors, containing bicyclic pyrrolo[1,2-c]imidazole framework, were prepared from N-(tert-butoxycarbonyl)-L-proline (1-Boc-L-proline). The sequential attachment of nitrogen nucleophiles and subsequent ring closure gave the desired bicyclic NHC precursors in good yields. The structures of these new NHC precursors were determined on the basis of spectroscopic techniques, including NMR and MS. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH

The Article related to bicyclic pyrroloimidazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Safety 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

On March 18, 2022, Tran, Duc N.; Zhdanko, Alexander; Barroso, Santiago; Nieste, Patrick; Rahmani, Ramdane; Holan, Jan; Hoefnagels, Roel; Reniers, Peter; Vermoortele, Frederik; Duguid, Stewart; Cazanave, Lionel; Figlus, Marek; Muir, Colin; Elliott, Alain; Zhao, Peichao; Paden, Warren; Diaz, Cristina Hernandez; Bell, Stephen J.; Hashimoto, Akihiro; Phadke, Avinash; Wiles, Jason A.; Vogels, Ilse; Farina, Vittorio published an article.Electric Literature of 79815-20-6 The title of the article was Development of a Commercial Process for Odalasvir. And the article contained the following:

Odalasvir is a selective inhibitor of hepatitis C virus NS5A protein, a key target for combination therapies. This paper described the chem. process development for the synthesis of this API and the improvements that were achieved over the medicinal chem. Optimization of all the reaction conditions and crystallizations resulted in higher throughput and a highly improved process mass intensity (PMI). The process was robust and it was scaled up to ∼100 kg batches without issues. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Electric Literature of 79815-20-6

The Article related to odalasvir preparation, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles 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 November 29, 2007, Teegarden, Bradley; Chapman, Dennis; Choi, Juyi; Feichtinger, Konrad; Han, Sangdon; Jayakumar, Honnappa; Tran, Thuy-Anh; Xu, Jingdong; Zou, Ning published a patent.Related Products of 52537-00-5 The title of the patent was Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto and their preparation. And the patent contained the following:

The present invention pertains to certain compounds of formula I and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy hypertension and pain. The invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered sep. or together. Compounds of formula I wherein X is O and S; V is O and NH; W and Z are independently (un)substituted C1-4 alkylene; R1 is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C3-7 cycloalkyl; R2 is H, C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkyl, etc.; R3 is H, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, carboxamide, CN, etc.; R4a is H, R4b is H, (un)substituted C1-12 acyl, (un)substituted carbo-C1-6 alkoxy, (un)substituted CO2-aryl, etc.; R5, R6 and R7 are independently H, C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkyl, etc.; R8 is (un)substituted C1-8 alkyl, (un)substituted (hetero)aryl, (un)substituted C3-10 cycloalkyl and (un)substituted heterocyclyl; and their pharmaceutically acceptable salts, hydrates, and solvates thereof, are claimed. Example compound II•TFA was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their 5-HT2A modulatory activity (some data given). 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 primary amine preparation 5ht2a serotonin receptor modulator treatment disease, pyrazolylphenyl amine preparation 5ht2a serotonin receptor modulator treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles 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