Day: November 3, 2022

De, Pinaki Bhusan; Banerjee, Sonbidya; Pradhan, Sourav; Punniyamurthy, Tharmalingam published an article in 2018, the title of the article was Ru(II)-Catalyzed C7-acyloxylation of indolines with carboxylic acids.SDS of cas: 52537-00-5 And the article contains the following content:

A method for the synthesis of 1-(pyrimidin-2-yl)indolin-7-yl-carboxylate derivative I [R = Ph, 2-thienyl, 1-naphthyl, etc.; R1 = H, 2-Me, 3-Me; R2 = H, 6-Cl, 4-Br, etc.] via ruthenium(II)-catalyzed site-selective C7-acyloxylation of indolines with carboxylic acids was presented. The substrate scope and functional group tolerance were important practical features. The kinetic isotope studies suggested that C-H bond activation might be the rate-determining step. 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 pyrimidinyl indolinyl carboxylate regioselective preparation, pyrimidyl indoline carboxylic acid acyloxylation ruthenium catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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 February 28, 1997, Arnold, Daniel Lee; Moyer, Mikel Paul; Sobolov-Jaynes, Susan Beth published a patent.SDS of cas: 52537-00-5 The title of the patent was Heterocyclic ring-fused pyrimidine derivatives, their intermediates and pharmaceutical compositions containing them. And the patent contained the following:

The invention refers to fused pyrimidines I [Y, together with the attached carbon atoms, form a 5- or 6-membered substituted aromatic ring, optionally containing 1-3 nitrogen atoms, and in addition optionally containing O or S; Z = NR1R2, Z’; R1 = H; R2 = Ph; R5 = various substituents, inc, heterocycles; R6 = OH, NH2, substituted amino, (un)substituted alkyl; n = 0, 1, 2; m = 1, 2, 3; dashed line = single or double bond], their stereoisomers and pharmaceutical medically acceptable salts and prodrugs. Thus, N-(3-ethynylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride II·HCl was prepared from 4-chloro-7H-pyrrolo[2,3-d]pyrimidine via amination with (3-aminophenyl)acetylene in pyridine followed by treatment with HCl in MeOH. These compounds inhibit the receptor tyrosine kinase enzymes and thus, they are able to selectively prevent the multiplication of breast cancer cells (no data). On the basis of this, they can be used to treat different hyperproliferative diseases, such as cancer of the lung, bladder, stomach, pancreas, liver, kidney, large intestine and rectum, as well as gynecol. cancers. In addition, they are suitable for the treatment of other non-cancerous hyperproliferative diseases, such as psoriasis, or non-malignant prostate hypertrophy. The invention also includes the pharmaceutical products that contain effectives doses of the general formula compounds as their active component, and the new intermediate products, which can be applied during the synthesis of the compounds according to the invention. 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 fused pyrimidine derivative preparation antiproliferative, psoriasis medicinal fused pyrimidine derivative, prostate hypertrophy medicinal fused pyrimidine derivative, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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

Ibrahem, Ismail; Zhao, Gui-Ling; Rios, Ramon; Vesely, Jan; Sunden, Henrik; Dziedzic, Pawel; Cordova, Armando published an article in 2008, the title of the article was One-pot organocatalytic domino Michael/α-alkylation reactions: direct catalytic enantioselective cyclopropanation and cyclopentanation reactions.Electric Literature of 79815-20-6 And the article contains the following content:

The development of one-pot organocatalytic domino Michael/α-alkylation reactions between bromomalonates or bromoacetoacetate esters and α,β-unsaturated aldehydes is presented. The chiral-amine-catalyzed reactions with bromomalonates as substrates give access to the corresponding 2-formylcyclopropane derivatives in high yields with excellent diastereoselectivity and up to 99% ee. The catalytic domino Michael/α-alkylation reactions between 4-bromo-acetoacetate and enals provide a route for the synthesis of functionalized cyclopentanones in good to high yields with 93-99% ee. The products from the organocatalytic reactions were also reduced with high diastereoselectivity to the corresponding cyclopropanols and cyclopentanols, resp. Moreover, one-pot combinations of amine and heterocyclic carbene catalysis (AHCC) enabled the highly enantioselective synthesis of β-malonate esters (91-97% ee) from the reaction between bromomalonates and enals. The tandem catalysis included the catalytic domino reaction followed by catalytic in situ chemoselective ring-opening of the 2-formylcyclopropane intermediates. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Electric Literature of 79815-20-6

The Article related to catalytic enantioselective cyclopropanation cyclopentanation, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction 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 1, 1986, Mitchell, Glynn; Rees, Charles W. published an article.Application of 65417-22-3 The title of the article was 1H-Azirines as intermediates in the photolysis of 1,2,3-triazoles. And the article contained the following:

Photolysis of triazoles I (R = 1-C10H7, R1 = H, R2 = CO2Et, CN; R1 = Me, R2 = CO2Me, CN) in MeCN gave the benzindoles II (R1, R2 as before) together with smaller amounts of the corresponding isomers III. Similarly, photolysis of I (R = Ph, R1 = H, Me, R2 = CO2Me) gave the rearranged products IV (R3 = CO2Me, R4 = H, Me) (V and VI, resp.) in 5 and 42% yield, resp., together with the isomeric IV (R3 = H, Me, R4 = CO2Me) in 25 and 21% yield, resp. Formation of II, V, and VI provides evidence for antiarom. 1H-azirines as reactive intermediates in a photochem. reaction. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Application of 65417-22-3

The Article related to triazole photolysis mechanism, azirine intermediate triazole photolysis, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction and other aspects.Application 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

Lakhdar, Sami; Appel, Roland; Mayr, Herbert published an article in 2009, the title of the article was How Does Electrostatic Activation Control Iminium-Catalyzed Cyclopropanations?.Related Products of 79815-20-6 And the article contains the following content:

Prediction of lg k=s(N+E) verified: In contrast to previous statements, ordinary α,β-unsaturated iminium ions do react with sulfur ylides. Electrostatic interactions accelerate the reactions by a factor of more than 105 and are responsible for the high stereoselectivity. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Related Products of 79815-20-6

The Article related to electrostatic activation iminium catalyzed cyclopropanation stereoselectivity, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction and other aspects.Related Products 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 16, 2005, Kunz, Roxanne K.; MacMillan, David W. C. published an article.Application In Synthesis of H-Idc-OH The title of the article was Enantioselective organocatalytic cyclopropanations. The identification of a new class of iminium catalyst based upon directed electrostatic activation. And the article contained the following:

A new method for enantioselective organocatalytic cyclopropanation is described. This study outlines the identification of a new class of iminium catalyst based on the concept of directed electrostatic activation (DEA). This novel organocatalytic mechanism exploits dual activation of ylide and enal substrates through a proposed electrostatic activation and stereodirected protocol. Formation of trisubstituted cyclopropanes with high levels of enantio- and diastereo-induction is accomplished for a variety of α,β-unsaturated aldehydes and sulfonium ylides. In addition, mechanistic studies have found that this cyclopropanation reaction exhibits enantioselectivity and reactivity profiles that are in accord with the proposed DEA step. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Application In Synthesis of H-Idc-OH

The Article related to enantioselective iminium organocatalyst cyclopropanation electrostatic activation, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction and other aspects.Application In Synthesis 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 September 30, 2014, Vakarov, S. A.; Gruzdev, D. A.; Chulakov, E. N.; Sadretdinova, L. Sh.; Ezhikova, M. A.; Kodess, M. I.; Levit, G. L.; Krasnov, V. P. published an article.Category: indole-building-block The title of the article was Diastereoselective Acylation of Racemic Heterocyclic Amines with N-Tosyl-(S)-Prolyl Chloride and its Structural Analogs. And the article contained the following:

A comparative study on the kinetic resolution of racemic amines (2,3-dihydro-4H-1,4-benzoxazine and 1,2,3,4-tetrahydroquinoline derivatives) by a diastereoselective acylation with N-tosyl-(S)-prolyl chloride and its structural analogs was performed. The effect of resolving agent structure on the stereoselectivity of heterocyclic amine acylation was examined The highest stereoselectivity was achieved in the case of acylation with acyl chlorides bearing a conformationally restricted pyrrolidine ring and an aromatic substituent in the protecting group at the nitrogen atom. The synthesis of the target compounds was achieved by a reaction of (2S)-1-[(4-methylphenyl)sulfonyl]-2-pyrrolidinecarbonyl chloride (proline chloride), (2S)-1-[(2-naphthalenyl)sulfonyl]-2-pyrrolidinecarbonyl chloride, (2S)-1-[(1-naphthalenyl)sulfonyl]-2-pyrrolidinecarbonyl chloride, (αS)-α-[methyl[(4-methylphenyl)sulfonyl]amino]benzenepropanoyl chloride, (2S)-tetrahydro-2-furancarbonyl chloride.(2S)-2,3-dihydro-1H-indole-2-carbonyl chloride with 7,8-difluoro-3,4-dihydro-3-methyl-2H-1,4-benzoxazine, 3,4-dihydro-3-methyl-2H-1,4-benzoxazine, 1,2,3,4-tetrahydro-2-methylquinoline. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Category: indole-building-block

The Article related to acyl chloride proline racemic amine acylation kinetic resolution, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) 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

Irvine, Robert W.; Summers, John C.; Taylor, Walter C. published an article in 1983, the title of the article was Photochemistry of dimethyl quinoline-3,4-dicarboxylate N-oxides.Safety of Methyl 2-methyl-1H-indole-3-carboxylate And the article contains the following content:

The photochem. rearrangement of di-Me 2-methyl- and 2-aryl-substituted quinoline-3,4-dicarboxylate N-oxides are examined In MeOH or MeOH-CHCl3 the major product was the 1-methyl- or 1-arylquinolin-2(1H)-one in which the substituent at C-2 has migrated to the N atom. The yield of these products was increased in a dark reaction subsequent to the irradiation In MeCN the inital major product was the corresponding 3,1-benzoxazepine; subsequent reactions yielded inter alia indole derivatives The intermediacy of fused oxaziridines or their ring opened isomeric zwittterions is discussed. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Safety of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to photochem rearrangement mechanism quinolinedicarboxylate oxide, Physical Organic Chemistry: Rearrangements, Including Isomerization and Tautomerization and other aspects.Safety of Methyl 2-methyl-1H-indole-3-carboxylate

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 12, 2013, Liu, Jin-Qiang; Cao, Xin-Xiang; Ji, Baoming; Zhao, Bangtun published an article.Name: H-Idc-OH The title of the article was Determination and Correlation of Solubilities of (S)-Indoline-2-carboxylic Acid in Six Different Solvents from (283.15 to 358.15) K. And the article contained the following:

The solubilities of (S)-indoline-2-carboxylilc acid (SIn2CA) in six pure solvents including water, methanol, ethanol, 1-propanol, 2-propanol, and 1-butanol were determined from (283.15 to 358.15) K at atm. pressure using the synthetic method. The solubility was determined by a laser monitoring observation technique and found to increase with the rise of temperature The exptl. solubilities were correlated by the modified Apelblat and λh (Buchowski) equations with the relative deviation less than 3.65% with the modified Apelblat equation and less than 0.023% with the λh equation. Thermodn. functions of the solution of SIn2CA in different solvents including apparent dissolution enthalpy and entropy were obtained by van’t Hoff equation, and the apparent dissolution Gibbs free energy change was also calculated The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Name: H-Idc-OH

The Article related to correlation solubility indolinecarboxylate water methanol ethanol propanol butanol, Phase Equilibriums, Chemical Equilibriums, and Solutions: Phase Equilibriums, Solubility and other aspects.Name: 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

Shi, Yao; Ke, Zhihai; Yeung, Ying-Yeung published an article in 2018, the title of the article was Environmentally benign indole-catalyzed position-selective halogenation of thioarenes and other aromatics.Category: indole-building-block And the article contains the following content:

An environmentally benign protocol for the synthesis of aryl bromides RBr [R = 3,4-di-MeOC6H3, 4-MeSC6H4, 2-Me-thienyl, etc.] was developed via regioselective electrophilic bromination of aromatic compounds Indole-catalyst was suitable for a wide range of substrates including thioarenes. 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 bromoarene green preparation regioselective, thioether bromination indole organocatalyst, arene bromination indole organocatalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Halides and Halonium Compounds 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