Author: Jessica.F

Ostrowski, Jacek published the artcilePharmacological and X-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats, HPLC of Formula: 125328-80-5, the main research area is androgen receptor modulator BMS564929 safety synthesis skeletal muscle prostate.

A novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (BMS-564929) has been identified, and this compound has been advanced to clin. trials for the treatment of age-related functional decline. BMS-564929 is a subnanomolar AR agonist in vitro, is highly selective for the AR vs. other steroid hormone receptors, and exhibits no significant interactions with SHBG or aromatase. Dose response studies in castrated male rats show that BMS-564929 is substantially more potent than testosterone (T) in stimulating the growth of the levator ani muscle, and unlike T, highly selective for muscle vs. prostate. Key differences in the binding interactions of BMS-564929 with the AR relative to the native hormones were revealed through x-ray crystallog., including several unique contacts located in specific helixes of the ligand binding domain important for coregulatory protein recruitment. Results from addnl. pharmacol. studies effectively exclude alternative mechanistic contributions to the observed tissue selectivity of this unique, orally active androgen. Because concerns regarding the potential hyperstimulatory effects on prostate and an inconvenient route of administration are major drawbacks that limit the clin. use of T, the potent oral activity and tissue selectivity exhibited by BMS-564929 are expected to yield a clin. profile that provides the demonstrated beneficial effects of T in muscle and other tissues with a more favorable safety window.

Endocrinology published new progress about Anabolism. 125328-80-5 belongs to class amides-buliding-blocks, name is N-(4-Bromo-3-chloro-2-methylphenyl)acetamide, and the molecular formula is C9H9BrClNO, HPLC of Formula: 125328-80-5.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Li, Chun-Tian published the artcileRearrangement of N-tert-Butanesulfinyl Enamines for Synthesis of Enantioenriched α-Hydroxy Ketone Derivatives, Formula: C4H11NOS, the main research area is acyclic tertiary hydroxy sulfenyloxy ketone preparation enantioselective; tert butanesulfinyl ketimine methyl triflate cascade enamination methylation rearrangement.

Treating chiral N-tert-butanesulfinyl ketimines with potassium hexamethyldisilazide (or potassium tert-butoxide) and Me triflate gives N-methylated N-tert-butanesulfinyl enamine intermediates that undergo stereoselective [2,3]-rearrangement to afford α-sulfenyloxy ketones I (R = Ph, iPr, 2-furyl, etc.; R’ = Me, allyl, Bn, etc.) with excellent enantiopurities. This cascade of enamination-N-methylation-rearrangement was even used to generate acyclic tertiary α-hydroxy ketones, II bearing two α-substituents showing negligible differences in bulkiness, such as Me and Et groups.

Organic Letters published new progress about Amination. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Formula: C4H11NOS.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Yang, Chu published the artcileAmination of Aromatic Halides and Exploration of the Reactivity Sequence of Aromatic Halides, HPLC of Formula: 123-39-7, the main research area is amination aromatic halide DMF amine reactivity.

A base-promoted amination of aromatic halides has been developed using a limited amount of DMF (DMF) or amine as an amino source. Various aryl halides, including F, Cl, Br, and I, have been successfully aminated in good to excellent yields. Although the amination of aromatic halides with amines or DMF is usually considered as an aromatic nucleophilic substitution (SNAr) process, and the reactivity of an aromatic halide is F > Cl > Br > I, the reactivity of aromatic halides in this system was found to be I > Br ≈ F > Cl. This protocol also showed a good regioselectivity for multihalogenated aromatics This protocol is valuable for industrial application due to the simplicity of operation, the unrestricted availability of amino sources and aromatic halides, transition metal-free conditions, no requirement for solvent, and scalability.

Journal of Organic Chemistry published new progress about Amination. 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, HPLC of Formula: 123-39-7.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhang, Yan published the artcileCu-Catalyzed carbamoylation versus amination of quinoline N-oxide with formamides, Category: amides-buliding-blocks, the main research area is copper catalyzed carbamoylation amination quinoline nitrogen oxide formamide; carbamoyl amino quinoline preparation cross dehydrogenative coupling radical mechanism.

An efficient, direct carbamoylation and amination of quinoline N-oxides with formamides to access 2-carbamoyl and 2-amino quinolines has been developed through copper-catalyzed C-C and C-N bond formations via cross-dehydrogenative coupling reactions. The reaction proceeds smoothly over a broad range of substrates with excellent functional group tolerance under mild conditions. Mechanistic studies suggest that the reaction is initiated by formamide radical or decarbonylative aminyl radical formation in the presence of TBHP, according to the different substituent on the N atom of formamide.

Organic & Biomolecular Chemistry published new progress about Amination. 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Song, Jia-Lin published the artcileRh(III)-Catalyzed N-Arylation of Alkyl Dioxazolones with Arylboronic Acids for the Synthesis of N-Aryl Amides, SDS of cas: 7465-88-5, the main research area is aryl amide preparation; alkyl dioxazolone aryl heterocyclic alkenyl boronic acid arylation amination.

Herein, a method for N-aryl amides preparation has been established through Rh(III)-catalyzed C(sp2)-N cross-coupling reactions of alkyl dioxazolones with arylboronic acids, heterocyclic boronic acid, and alkenyl boronic acid. This efficient and straightforward catalytic approach was featured with broad substrate scope (38 examples), good functional group compatibility, high yields (up to 99 %), and is suitable for late-stage modification of drug mol. structures. The possible mechanism hypothesis was also accomplished.

European Journal of Organic Chemistry published new progress about Amination. 7465-88-5 belongs to class amides-buliding-blocks, name is 4-Methoxy-N-phenylbenzamide, and the molecular formula is C14H13NO2, SDS of cas: 7465-88-5.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kawada, Takuma published the artcileAsymmetric Transfer Hydrogenative Amination of Benzylic Ketones Catalyzed by Cp*Ir(III) Complexes Bearing a Chiral N-(2-Picolyl)sulfonamidato Ligand, Category: amides-buliding-blocks, the main research area is amine preparation chemoselective diastereoselective enantioselective; benzylic ketone asym transfer hydrogenative amination iridium complex catalyst.

A convenient asym. reductive amination of benzylic ketones (α-arylated ketones) catalyzed by newly designed Cp*Ir complexes bearing a chiral N-(2-picolyl)sulfonamidato ligand was developed. Using readily available β-amino alcs. as chiral aminating agents, a range of benzo-fused and acyclic ketones were successfully reduced with formic acid in methanol at 40°C to afford amines with favorable chemo- and diastereoselectivities. The amino alc.-derived chiral auxiliary was easily removed by mild periodic oxidants, leading to optically active primary β-arylamines without erosion of the optical purity (up to 97% ee). The excellent catalytic performance was retained even upon lowering the amount of catalyst to a substrate/catalyst (S/C) ratio of 20,000, and the amination could be performed on a large scale exceeding 100 g. The precise hydride transfer to iminium species generated from the ketonic substrate and the chiral amine counterpart was suggested by the mechanistic studies on stoichiometric reactions of isolable hydridoiridium complexes and model intermediates such as N,O-acetal, enamine, and iminium compounds

Journal of Organic Chemistry published new progress about Amination. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Liu, Xinwei published the artcileH2O2 -promoted C-C bond oxidative cleavage of β-O-4 lignin models to benzanilides using water as a solvent under metal-free conditions, Recommanded Product: 4-Methoxy-N-phenylbenzamide, the main research area is lignin model bond cleavage benzanilide hydrogen peroxide water solvent.

The production of aromatic compounds from lignin is an essential issue in the transformation of biomass. Herein, a simple method has been presented for the synthesis of benzanilides and phenols from aniline involving the oxidative cleavage of β-O-4 lignin models using H2O2 as an oxidizing agent without any metal catalysts and under relatively mild conditions.

Green Chemistry published new progress about Amidation. 7465-88-5 belongs to class amides-buliding-blocks, name is 4-Methoxy-N-phenylbenzamide, and the molecular formula is C14H13NO2, Recommanded Product: 4-Methoxy-N-phenylbenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhang, Shu-Wei published the artcileSynthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors, Product Details of C4H11NOS, the main research area is bisthiazole derivative preparation anticancer HDAC inhibitor.

A series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors was developed during our previous work. In the present work, a new series of highly potent bisthiazole-based compounds were designed and synthesized. Among the prepared compounds, compound I, which contains an α-(S)-methyl-substituted benzyl group, displays potent inhibitory activity toward human HDACs and several cancer cells lines. Compound I has a favorable PK profile and high tissue distribution specificity in the colon, as well as good efficacy in the AOM-DSS mouse model for colitis-associated colonic tumorigenesis.

Journal of Medicinal Chemistry published new progress about Amidation. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Product Details of C4H11NOS.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Ghamari kargar, Pouya published the artcileA porous metal-organic framework (Ni-MOF): An efficient and recyclable catalyst for cascade oxidative amidation of alcohols by amines under ultrasound-irradiations, Application of 4-Methoxy-N-phenylbenzamide, the main research area is nickel metal organic framework surface area amidation green chem.

A novel and green protocol was developed for the synthesis of amides via the reaction of benzyl alcs. with amines in the presence of Ni-MOF named UoB-8 as catalyst. The morphol., structural, and physicochem. characteristics of the Ni-MOF were investigated by FT-IR, XRD, FESEM, EDX, TEM, BET, CHN and ICP analyses. The products were obtained in good to excellent yields, with short reaction times, under ultrasound irradiation (40 °C) in ethanol as solvent. In addition, low-cost catalyst was recovered and reused at least 5 times without detecting a noticeable reduction in efficiency.

Molecular Catalysis published new progress about Amidation. 7465-88-5 belongs to class amides-buliding-blocks, name is 4-Methoxy-N-phenylbenzamide, and the molecular formula is C14H13NO2, Application of 4-Methoxy-N-phenylbenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Li, Guangchen published the artcileHighly Chemoselective, Transition-Metal-Free Transamidation of Unactivated Amides and Direct Amidation of Alkyl Esters by N-C/O-C Cleavage, Recommanded Product: 4-Methoxy-N-phenylbenzamide, the main research area is chemoselective transamidation unactivated amide amidation alkyl ester.

The amide bond is one of the most fundamental functional groups in chem. and biol. and plays a central role in numerous processes harnessed to streamline the synthesis of key pharmaceutical and industrial mols. Although the synthesis of amides is one of the most frequently performed reactions by academic and industrial scientists, the direct transamidation of tertiary amides is challenging due to unfavorable kinetic and thermodn. contributions of the process. Herein, we report the first general, mild, and highly chemoselective method for transamidation of unactivated tertiary amides by a direct acyl N-C bond cleavage with non-nucleophilic amines. This operationally simple method is performed in the absence of transition metals and operates under unusually mild reaction conditions. In this context, we further describe the direct amidation of abundant alkyl esters to afford amide bonds with exquisite selectivity by acyl C-O bond cleavage. The utility of this process is showcased by a broad scope of the method, including various sensitive functional groups, late-stage modification, and the synthesis of drug mols. (>80 examples). Remarkable selectivity toward different functional groups and within different amide and ester electrophiles that is not feasible using existing methods was observed Extensive exptl. and computational studies were conducted to provide insight into the mechanism and the origins of high selectivity. We further present a series of guidelines to predict the reactivity of amides and esters in the synthesis of valuable amide bonds by this user-friendly process. In light of the importance of the amide bond in organic synthesis and major practical advantages of this method, the study opens up new opportunities in the synthesis of pivotal amide bonds in a broad range of chem. contexts.

Journal of the American Chemical Society published new progress about Amidation. 7465-88-5 belongs to class amides-buliding-blocks, name is 4-Methoxy-N-phenylbenzamide, and the molecular formula is C14H13NO2, Recommanded Product: 4-Methoxy-N-phenylbenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics