Tag: 200-300

On February 28, 2002, Meyers, Jason K.; Rogers, Bruce N.; Groppi, Vincent E., Jr.; Piotrowski, David W.; Bodnar, Alice L.; Jacobsen, Eric Jon; Corbett, Jeffrey W. published a patent.Product Details of 400715-69-7 The title of the patent was Preparation of N-quinuclidinyl-heteroaryl amides for pharmaceutical use in the treatment of neurological disorders. And the patent contained the following:

N-quinuclidinyl-heteroaryl amides, such as I [R1 = H, alkyl, cycloalkyl, haloalkyl, aryl; R2 = H, benzyl, alkyl, haloalkyl, cycloalkyl, aryl; W = heteroaryl; X = O, S], were prepared for therapeutic use in the treatment of neurol. disorders, such as cognitive and attention deficit symptoms of Alzheimer’s, neurodegeneration associated with diseases such as Alzheimer’s disease, pre-senile dementia (mild cognitive impairment), or senile dementia. Thus, the hydrochloride salt of quinuclidine carboxamide II was prepared in 57% yield by an amidation reaction of (3R)-3-aminoquinuclidine hydrochloride and 5-phenylthiophene-2-carboxylic acid using di-Ph chlorophosphate and Et3N in CH2Cl2 and DMF/H2O (5:1). The prepared quinuclidinyl amides were tested for nicotinic acetylcholine receptor binding activities. The experimental process involved the reaction of Ethyl 5-(3-chlorophenyl)oxazole-2-carboxylate(cas: 400715-69-7).Product Details of 400715-69-7

The Article related to quinuclidine heteroaryl preparation neurol disorder treatment, alzheimer disease treatment quinuclidine heteroaryl preparation, dementia treatment quinuclidine heteroaryl preparation, nicotinic receptor binding quinuclidine heteroaryl preparation and other aspects.Product Details of 400715-69-7

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On February 28, 2002, Myers, Jason K.; Rogers, Bruce N.; Groppi, Vincent E., Jr.; Piotrowski, David W.; Bodnar, Alice L.; Jacobsen, Eric Jon; Corbett, Jeffrey W. published a patent.Computed Properties of 400715-69-7 The title of the patent was Preparation of N-quinuclidinyl-heteroaryl amides for pharmaceutical use in the treatment of neurological disorders. And the patent contained the following:

N-quinuclidinyl-heteroaryl amides, such as I [R1 = H, alkyl, cycloalkyl, haloalkyl, aryl; R2 = H, benzyl, alkyl, haloalkyl, cycloalkyl, aryl; W = heteroaryl; X = O, S], were prepared for therapeutic use in the treatment of neurol. disorders, such as attention deficit disorder, attention deficit hyperactivity disorder, mood and affective disorders, amyotrophic lateral sclerosis, borderline personality disorder, traumatic brain injury, behavioral and cognitive problems associated with brain tumors, AIDS dementia complex, dementia associated with Down’s syndrome, dementia associated with Lewy Bodies, Huntington’s disease, depression, general anxiety disorder, age-related macular degeneration, Parkinson’s disease, tardive dyskinesia, Pick’s disease, post traumatic stress disorder, dysregulation of food intake including bulimia and anorexia nervosa, withdrawal symptoms associated with smoking cessation and dependent drug cessation, Gilles de la Tourette’s Syndrome, glaucoma, neurodegeneration associated with glaucoma, or symptoms associated with pain. Thus, the hydrochloride salt of quinuclidine carboxamide II was prepared in 57% yield by an amidation reaction of (3R)-3-aminoquinuclidine hydrochloride and 5-phenylthiophene-2-carboxylic acid using di-Ph chlorophosphate and Et3N in CH2Cl2 and DMF/H2O (5:1). The prepared quinuclidinyl amides were tested for nicotinic acetylcholine receptor binding activities. The experimental process involved the reaction of Ethyl 5-(3-chlorophenyl)oxazole-2-carboxylate(cas: 400715-69-7).Computed Properties of 400715-69-7

The Article related to quinuclidine heteroaryl preparation neurol disorder treatment, alzheimer disease treatment quinuclidine heteroaryl preparation, dementia treatment quinuclidine heteroaryl preparation, nicotinic receptor binding quinuclidine heteroaryl preparation and other aspects.Computed Properties of 400715-69-7

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On May 14, 2020, Shepard, Stacey; Combs, Andrew P. published a patent.SDS of cas: 877149-10-5 The title of the patent was Preparation of heterocyclic derivatives as PI3K inhibitors. And the patent contained the following:

This invention relates to compounds I [Z = CZ1 or N; Z1 and R12 = (independently) H, D, OH, NO2, etc.; R1 = H, D, halo, alkyl, etc.; R2 = H, D, halo, alkyl, etc.; R6 = H, D, halo, alkyl, etc.; X9 = (un)substituted NH or CH2; X11 = (un)substituted NH or CH2; R = H, alkyl, alkenyl, etc.] or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases. E.g., a multi-step synthesis of (S)-II, starting from 4-bromopyridine-2-carbonitrile, was disclosed. The exemplified compounds I were tested in the PI3Kγ, PI3Kδ, and PI3Kγ THP1 RPS6 ELISA assays (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of Methyl 4-bromo-2-chloro-6-methylbenzoate(cas: 877149-10-5).SDS of cas: 877149-10-5

The Article related to heterocyclic derivative preparation pi3k gamma inhibitor antitumor cardiovascular, autoimmune neurodegenerative disease treatment heterocyclic derivative preparation pi3k gamma, heteroarylpyridazinyl heteroarylpyridyl isoindolinone indazole preparation pi3k gamma inhibitor and other aspects.SDS of cas: 877149-10-5

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On March 23, 2022, Varkhedkar, Rajesh; Yang, Fan; Dontha, Rakesh; Zhang, Jianglin; Liu, Jiyong; Spingler, Bernhard; van der Veen, Stijn; Duttwyler, Simon published an article.HPLC of Formula: 14602-86-9 The title of the article was Natural-Product-Directed Catalytic Stereoselective Synthesis of Functionalized Fused Borane Cluster-Oxazoles for the Discovery of Bactericidal Agents. And the article contained the following:

The identification of an alternative chem. space to address the global challenge posed by emerging antimicrobial resistance is very much needed for the discovery of novel antimicrobial lead compounds B clusters are currently being explored in drug discovery due to their unique steric and electronic properties. However, the challenges associated with the synthesis and derivatization techniques of these compounds have limited their utility in the rapid construction of a library of mols. for screening against various biol. targets as an alternative mol. platform. Herein, the authors report a transition-metal-catalyzed regioselective direct B-H alkylation-annulation of the closo-dodecaborate anion with natural products such as menthol and camphor as the directing groups. This method allowed the rapid construction of a library of 1,2,3-trisubstituted clusters, which were evaluated in terms of their antibacterial activity against WHO priority pathogens. Several of the synthesized dodecaborate derivatives displayed medium- to high-level bactericidal activity against Gram-pos. and Gram-neg. bacteria. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).HPLC of Formula: 14602-86-9

The Article related to mentholdiboraoxazole fused carborane preparation antibacterial activity, crystal structure mentholdiboraoxazole fused carborane, mol structure mentholdiboraoxazole fused carborane, rhodium catalyzed regioselective alkylation annulation dodecaborate anion styrene derivative and other aspects.HPLC of Formula: 14602-86-9

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On June 3, 2016, Castanheiro, Thomas; Suffert, Jean; Gulea, Mihaela; Donnard, Morgan published an article.Application of 14602-86-9 The title of the article was Aerobic Copper-Mediated Domino Three-Component Approach to 2-Aminobenzothiazole Derivatives. And the article contained the following:

N-(2-Benzothiazolyl)amides were prepared by the three-component reactions of 2,2′-diaminodiaryl disulfides (or the hydrochloride of an aminotrifluoromethylbenzenethiol), copper cyanide, and acyl, dimethylthiocarbamoyl, or L-menthyloxyformyl chlorides, Boc anhydride, and Ph isocyanate using an oxidative copper-mediated S-cyanation as a key step followed by cyclization and acylation. The reaction proceeds by a mechanism involving an intermol. migration of the acyl group, as scrambling of acyl groups in reactions of acylaminophenyl disulfides was found. The structure of N-(2-benzothiazolyl)-2,5-difluorobenzamide was determined by X-ray crystallog. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Application of 14602-86-9

The Article related to benzothiazolyl amide chemoselective preparation, copper cyanide aminoaryl disulfide thiol acyl chloride chemoselective reaction, oxidative cyanation cyclization acylation reaction copper cyanide aminoaryl disulfide, fluorobenzamide benzothiazolyl mol crystal structure and other aspects.Application of 14602-86-9

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Cui, Ji-Bin; Wei, Xiao-Xiong; Zhao, Rui; Zhu, Huixia; Shi, Jing; Bierer, Donald; Li, Yi-Ming published an article in 2021, the title of the article was Chemical synthesis of disulfide surrogate peptides by using beta-carbon dimethyl modified diaminodiacids.Name: tert-Butyl trichloroacetimidate And the article contains the following content:

The replacement of disulfide bridges with metabolically stable isosteres is a promising strategy to improve the stability of disulfide-rich polypeptides towards reducing agents and isomerases. A diaminodiacid-based strategy is one of the most effective methods to construct disulfide bond mimics, but modified diaminodiacids have not been developed till now. Inspired by the fact that alkylation of disulfide bonds can regulate the activity of polypeptides, herein, we report the first example of thioether bridged diaminodiacids incorporating Cys Cβ di-Me modification, obtained by penicillamine (Pen)-based thiol alkylation. The utility of these new diaminodiacids was demonstrated by the synthesis of disulfide surrogates of oxytocin containing a short-span disulfide bond and of KIIIA with large-span disulfide bonds. This new type of synthetic bridge further extends the diaminodiacid toolbox to facilitate the study of the structure-activity relationship of disulfide-rich peptides. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Name: tert-Butyl trichloroacetimidate

The Article related to peptide disulfide surrogate synthesis betacarbon dimethyl diaminodiacid, penicillamine thiol disulfide bond alkylation steric hindrance, oxytocin disulfide surrogates synthesis conotoxin kiiia analog, solid phase peptide synthesis oxidative cyclization ncl folding and other aspects.Name: tert-Butyl trichloroacetimidate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On June 5, 2020, Shabani, Sadegh; Hutton, Craig A. published an article.Recommanded Product: tert-Butyl trichloroacetimidate The title of the article was Total synthesis of Seongsanamide B. And the article contained the following:

The first total synthesis of the bicyclic depsipeptide natural product seongsanamide B is described. The successful approach employed solid-phase peptide synthesis of a core heptapeptide, incorporating on-resin esterification, followed by solution-phase macrolactamization and a late stage intramol. Evans-Chan-Lam coupling to generate the biaryl ether of the isodityrosine unit. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: tert-Butyl trichloroacetimidate

The Article related to bicyclic depsipeptide natural product seongsanamide b total synthesis, seongsanamide natural product antiallergic agent drug, solid phase synthesis peptide coupling heptapeptide esterification macrolactamization, evans chan lam coupling isodityrosine biaryl ether and other aspects.Recommanded Product: tert-Butyl trichloroacetimidate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On May 6, 2016, Vincent, Adrien; Deschamps, Damien; Martzel, Thomas; Lohier, Jean-Francois; Richards, Christopher J.; Gaumont, Annie-Claude; Perrio, Stephane published an article.SDS of cas: 14602-86-9 The title of the article was Enantiomerically Pure [2.2]Paracyclophane-4-thiol: A Planar Chiral Sulfur-Based Building Block Readily Available by Resolution with an Amino Acid Chiral Auxiliary. And the article contained the following:

Acyl chloride of N-phthaloyl-(S)-isoleucine is an efficient chiral auxiliary for the resolution of (±)-[2.2]paracyclophane-4-thiol. A preparative protocol, based on the conversion into diastereoisomeric thiolesters and separation by two fractional crystallizations and column chromatog., was developed. Deprotection with LiAlH4 allowed isolation of the individual thiol enantiomers in good yield (∼40%) and high enantiomeric purity (ee >93%). The absolute configurations were determined by comparison of the optical rotation value of the products with literature data and were confirmed by X-ray crystallog. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).SDS of cas: 14602-86-9

The Article related to chiral paracyclophane thiol preparation resolution amino acid auxiliary, acyl chloride phthaloyl isoleucine auxiliary preparation paracyclophane resolution, crystal mol structure paracyclophane thiol, phthaloyl leucine auxiliary preparation crystal mol structure and other aspects.SDS of cas: 14602-86-9

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On September 4, 2020, He, Tingting; Peng, Lei; Li, Shan; Hu, Fangli; Xie, Chuandong; Huang, Shengli; Jia, Shiqi; Qin, Wenling; Yan, Hailong published an article.Product Details of 98946-18-0 The title of the article was Chiral Naphthyl-C2-Indole as Scaffold for Phosphine Organocatalysis: Application in Asymmetric Formal [4 + 2] Cycloaddition Reactions. And the article contained the following:

The applications of a newly designed chiral naphthyl-C2-indole bifunctional phosphine organocatalyst I in stereoselective formal [4 + 2] cycloaddition reactions were reported. The chiral naphthyl-C2-indole skeleton was introduced to bifunctional phosphine organocatalysis for the first time, and excellent stereocontrol was achieved in formal [4 + 2] cycloaddition reactions of dicyanomethyleneoxindoles II (R1 = Me, MeOCH2, H2C:CHCH2, PhCH2, Ph; R2 = H, 5-Me, 7-Me, 6-MeO, 6-MeO, 7-F3C, 5-Cl, 5-Br, 6-Br) with pentadienones (E)-R3CH:CHCOCH:CH2 (R3 = Ph, 4-MeC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 2-furyl) and of oxoindolylideneacetates III (R4 = H, Me, MeOCH2, H2C:CHCH2, Boc, Ph, PhCH2, PhCO; R5 = H, 5-Me, 7-Me, 5, 7-Me2, 5-MeO, 6-MeO, 5-F, 5-Cl, 6-Cl, 5-Br, 6-Br, 7-Br; X = CH, N) with 3-acryloylbenzofuran. With the optimal catalyst, chiral spirooxindoles IV (R1 = Me, MeOCH2, H2C:CHCH2, PhCH2, Ph; R2 = H, 5-Me, 7-Me, 6-MeO, 6-MeO, 7-F3C, 5-Cl, 5-Br, 6-Br; R3 = Ph, 4-MeC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 2-furyl) and spirodibenzofuranoxindoles V (R4 = H, Me, MeOCH2, H2C:CHCH2, Boc, Ph, PhCH2, PhCO; R5 = H, 5-Me, 7-Me, 5, 7-Me2, 5-MeO, 6-MeO, 5-F, 5-Cl, 6-Cl, 5-Br, 6-Br, 7-Br; X = CH, N) were produced in moderate to good yields with excellent stereoselectivities (up to >99% ee, >20:1 dr). The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0

The Article related to phosphinoindolylnaphthol nonracemic preparation organocatalyst, spirooxindole spirodibenzofuranoxindole diastereoselective enantioselective preparation, stereoselective formal cycloaddition dicyanomethyleneoxindole pentadienone phosphinoindolylnaphthol catalyst and other aspects.Product Details of 98946-18-0

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Schlauderer, Florian; Lammens, Katja; Nagel, Daniel; Vincendeau, Michelle; Eitelhuber, Andrea C.; Verhelst, Steven H. L.; Kling, Dale; Chrusciel, Al; Ruland, Juergen; Krappmann, Daniel; Hopfner, Karl-Peter published an article in 2013, the title of the article was Structural Analysis of Phenothiazine Derivatives as Allosteric Inhibitors of the MALT1 Paracaspase.Category: chlorides-buliding-blocks And the article contains the following content:

The authors report the crystal structure of ligand-free dimeric human MALT1casp-Ig3 in complex with the tricyclic phenothiazine derivative thioridazine. Unexpectedly, the structure reveals that the inhibitor binds in a pocket located on the opposite to the caspase active site, in the interface between the caspase domain and the Ig3 domain connecting helix α1Ig3 of MALT1. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Category: chlorides-buliding-blocks

The Article related to phenothiazine malt1 paracaspase allosteric inhibitor crystal mol structure design, antitumor multiple sclerosis enzyme inhibitor design phenothiazine derivative prepare, enantiomer resolution phenothiazine malt1 paracaspase allosteric inhibitor mol docking, cancer, inhibitors, medicinal chemistry, multiple sclerosis, thioridazine and other aspects.Category: chlorides-buliding-blocks

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics