Tag: M.W=150-200

Lewis, Frank W.; Bird, Kathleen; Navarro, Jean-Philippe; El Fallah, Rawa; Brandel, Jeremy; Hubscher-Bruder, Veronique; Tsatsanis, Andrew; Duce, James A.; Tetard, David; Bourne, Samuel; Maina, Mahmoud; Pienaar, Ilse S. published the artcile< Synthesis, physicochemical characterization and neuroprotective evaluation of novel 1-hydroxypyrazin-2(1H)-one iron chelators in an in vitro cell model of Parkinson′s disease>, Recommanded Product: H-Leu-OEt.HCl, the main research area is Parkinson disease iron chelator physicochem property neuroprotective.

Iron dysregulation, dopamine depletion, cellular oxidative stress and α-synuclein protein mis-folding are key neuronal pathol. features seen in the progression of Parkinson′s disease. Iron chelators endowed with one or more therapeutic modes of action have long been suggested as disease modifying therapies for its treatment. In this study, novel 1-hydroxypyrazin-2(1H)-one iron chelators were synthesized and their physicochem. properties, iron chelation abilities, antioxidant capacities and neuroprotective effects in a cell culture model of Parkinson′s disease were evaluated. Physicochem. properties (log β, log D7.4, pL0.5) suggest that these ligands have a poorer ability to penetrate cell membranes and form weaker iron complexes than the closely related 1-hydroxypyridin-2(1H)-ones. Despite this, we show that levels of neuroprotection provided by these ligands against the catecholaminergic neurotoxin 6-hydroxydopamine in vitro were comparable to those seen previously with the 1-hydroxypyridin-2(1H)-ones and the clin. used iron chelator Deferiprone, with two of the ligands restoring cell viability to ≥89% compared to controls. Two of the ligands were endowed with addnl. phenol moieties in an attempt to derive multifunctional chelators with dual iron chelation/antioxidant activity. However, levels of neuroprotection with these ligands were no greater than ligands lacking this moiety, suggesting the neuroprotective properties of these ligands are due primarily to chelation and passivation of intracellular labile iron, preventing the generation of free radicals and reactive oxygen species that otherwise lead to the neuronal cell death seen in Parkinson′s disease.

Dalton Transactions published new progress about Antioxidants. 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Recommanded Product: H-Leu-OEt.HCl.

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

Yang, Huan; Zhang, Li; Zhou, Fei-Yu; Jiao, Lei published the artcile< An umpolung approach to the hydroboration of pyridines: a novel and efficient synthesis of N-H 1,4-dihydropyridines>, Computed Properties of 33402-75-4, the main research area is diboron pyridine inverse hydroboration deuteration; dihydropyridine preparation.

The first inverse hydroboration of pyridine with a diboron compound and a proton source was realized under simple basic and catalyst-free conditions. This process consisted of a formal boryl anion addition to pyridine, which produced an N-boryl pyridyl anion complex and the subsequent protonation of the anion complex. This process enabled a simple and efficient method for the synthesis of multi-substituted N-H 1,4-dihydropyridine (1,4-DHP) derivatives that were difficult to prepare using established methods. Furthermore, this method allowed facile preparation of 4-deuterated 1,4-DHPs from an easily accessible deuterium ion source. This inverse hydroboration reaction represented a new mode for pyridine functionalization.

Chemical Science published new progress about Deuteration, regioselective. 33402-75-4 belongs to class esters-buliding-blocks, and the molecular formula is C8H9NO2, Computed Properties of 33402-75-4.

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

Loro, Camilla; Molteni, Letizia; Papis, Marta; Lo Presti, Leonardo; Foschi, Francesca; Beccalli, Egle M.; Broggini, Gianluigi published the artcile< Non-Decarboxylative Ruthenium-Catalyzed Rearrangement of 4-Alkylidene-isoxazol-5-ones to Pyrazole- and Isoxazole-4-carboxylic Acids>, Safety of Ethyl 3-oxo-3-phenylpropanoate, the main research area is pyrazole carboxylic acid preparation; hydroaminoalkylidenyl isoxazolone rearrangement ruthenium catalyst; isoxazole carboxylic acid preparation; hydroxyalkylidenyl isoxazolone rearrangement ruthenium catalyst.

Non-decarboxylative ruthenium-catalyzed rearrangement of 4-(2-hydroaminoalkylidenyl)- and 4-(2-hydroxyalkylidenyl)-substituted isoxazol-5(4H)-ones with catalytic amounts of [RuCl2(p-cymene)]2, without any additive, afforded pyrazole-4-carboxylic acids I [R1 = Me, Pr, Ph, etc.; R2 = H, Me, Et, etc.; R3 = Ph, CH2Bn, etc.] and isoxazole-4-carboxylic acids I [R1 = Me, Pr, Ph, etc.; R2 = H, Me, Ph, etc.] resp. The presence of an intramol. H-bond in these substrates was the key to divert the classical mechanism toward a ring-opening non-decarboxylative path that was expected to generate a vinyl Ru-nitrenoid intermediate, the cyclization of which afforded the rearranged products I and II. A gram scale protocol demonstrated the synthetic applicability of this transformation.

Organic Letters published new progress about Alkylidenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 94-02-0 belongs to class esters-buliding-blocks, and the molecular formula is C11H12O3, Safety of Ethyl 3-oxo-3-phenylpropanoate.

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

Boerjesson, Lena; Welch, Christopher J. published the artcile< Synthesis of 2-hydroxymethyl-1-oxaquinolizidine>, Application In Synthesis of 617-55-0, the main research area is hydroxymethyloxaquinolizidine stereoselective preparation; oxaquinolizidinemethanol stereoselective preparation.

(2S,5R,10S)-2-Hydroxymethyl-1-oxaquinolizidine, a xestospongine intermediate, was prepared stereospecifically from L-malic acid and 1,5-pentanediol.

Tetrahedron published new progress about 617-55-0. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Application In Synthesis of 617-55-0.

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

Li, Bing; Williams, John D.; Peet, Norton P. published the artcile< Two concise total syntheses of the wasabi phytoalexin methyl 1-methoxyindole-3-carboxylate>, Formula: C9H9NO4, the main research area is nitrophenylacrylate preparation reductive cyclization; wasabi phytoalexin methoxyindolecarboxylate total synthesis.

Two new syntheses of the phytoalexin Me 1-methoxyindole-3-carboxylate (I) were developed that employ the same key intermediate. Me 2-(2-nitrophenyl)acrylate (II) was directly converted into I using modified Cadogan-Sundberg indole synthesis conditions with P(OMe)3. Acrylate II also underwent reductive cyclization with SnCl2 to give Me 1-hydroxyindole-3-carboxylate, which was methylated to produce I.

Tetrahedron Letters published new progress about Reductive cyclization. 30095-98-8 belongs to class esters-buliding-blocks, and the molecular formula is C9H9NO4, Formula: C9H9NO4.

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

Wiesler, Stefan; Bau, Michael A.; Niepel, Thomas; Younas, Sara L.; Luu, Hieu-Trinh; Streuff, Jan published the artcile< Synthesis of α,ω-Bis-Enones by the Double Addition of Alkenyl Grignard Reagents to Diacid Weinreb Amides>, Safety of (S)-Dimethyl 2-hydroxysuccinate, the main research area is enone preparation double addition alkenyl Grignard diacid Weinreb amide.

An efficient double addition of substituted alkenylmagnesium bromides to bis-Weinreb amides has been developed, giving α,ω-bis-enones that are building blocks for certain drugs and polymers. Furthermore, reliable protocols for the preparation of the required substituted alkenylmagnesium reagents from substituted non-activated alkenyl bromides are reported. The double addition is demonstrated on 25 examples, including enantiopure as well as conjugated and cross-conjugated bis-enones. The addition to a cyclohexane-1,2-dicarboxamide was found to lead to a selective mono addition, giving access to cyclohexyl γ-ketoamides that are core motifs of several pharmaceutical agents and promising drug candidates.

European Journal of Organic Chemistry published new progress about Addition reaction (double). 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Safety of (S)-Dimethyl 2-hydroxysuccinate.

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

de Ancos, Begona; Maestro, M. Carmen; Martin, M. Rosario; Mateo, Ana I. published the artcile< Reactions of pyrrolidine enamines of cyclic and acyclic 3,4-dioxobutanoic acid derivatives with dimethyl acetylenedicarboxylate. A new case of atropisomerism>, Recommanded Product: Methyl 4,4-dimethoxy-3-oxobutanoate, the main research area is pyrrolidine enamine reaction acetylenedicarboxylate atropisomerism.

Reaction conditions and structure of the starting enamines (cyclic or open-chain) determine greatly the final products of the title reactions. Whereas in benzene and acetonitrile, MeO2CCCCO2Me and pyrrolidinylbutanoate I give a mixture of the diastereoisomeric dienamines II, in methanol I affords pyrrolizine III. Enaminofuranones IV (R = Me, menthyl, R1 = H) furnish the corresponding “”Michael adducts”” (E)- and (Z)-IV and V but fail to yield pyrrolizines.

Tetrahedron published new progress about Atropisomers. 60705-25-1 belongs to class esters-buliding-blocks, and the molecular formula is C7H12O5, Recommanded Product: Methyl 4,4-dimethoxy-3-oxobutanoate.

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

Zhulanov, Vladimir E.; Vigovskaya, Valeria A.; Dmitriev, Maksim V.; Silaichev, Pavel S.; Maslivets, Andrey N.; Rubin, Michael published the artcile< Dipyrazolodioxadiazocines as shelf-stable ""ready-to-use"" precursors for an in situ generation of enolate-iminium 1,4-dipoles: a straightforward atom-economical approach to pyrazolo[5,1-d][1,3,5]dioxazines>, HPLC of Formula: 94-02-0, the main research area is pyrazolodioxazine preparation atom economy; dipyrazolodioxadiazocine ketone heterocyclization insitu generated cyclic enolate iminium dipole.

An original, facile and highly efficient method for the in situ generation of cyclic enolate-iminium 1,4-dipoles via unique thermal decomposition of easily available dipyrazolodioxadiazocines was developed. Various substituted pyrazolo[5,1-d][1,3,5]dioxazines I [R1 = COOEt, PhCO, 4-MeC6H4CO, 4-ClC6H4CO; R2 = CO2Me, Ph; R3 = Me, Et; R4 = Et, t-Bu, n-Bu, i-Bu, Bn; R3R4 = (CH2)4, (CH2)5, (CH2)6, etc.] were prepared in high yields via unusual cycloconversion of dipyrazolodioxadiazocines in the presence of ketones. Furthermore, the developed method was 100% atom economical and proceeds under metal-, catalyst- and solvent-free conditions.

Organic & Biomolecular Chemistry published new progress about Atom economy. 94-02-0 belongs to class esters-buliding-blocks, and the molecular formula is C11H12O3, HPLC of Formula: 94-02-0.

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

Poupardin, Olivia; Greck, Christine; Genet, Jean Pierre published the artcile< Efficient asymmetric synthesis of a functionalized Δ2-pyrazoline>, Category: esters-buliding-blocks, the main research area is pyrazolinecarboxylate asym synthesis.

The asym. synthesis of Me (4S,5R)-4-hydroxy-3-pyrazoline-5-carboxylate in 4 steps is described starting from 4,4-dimethoxy-3-oxobutanoate by sequential catalytic hydrogenation and electrophilic amination.

Tetrahedron Letters published new progress about Stereoselective synthesis. 60705-25-1 belongs to class esters-buliding-blocks, and the molecular formula is C7H12O5, Category: esters-buliding-blocks.

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

Thiam, Mohamadou; Slassi, Abdelmalik; Chastrette, Francine; Amouroux, Roger published the artcile< Malic acid as a chiral synthon: synthesis of 1,2 and 1,3 optically active diols>, Name: (S)-Dimethyl 2-hydroxysuccinate, the main research area is chiral synthon malic acid; diol optically active.

Com. malic acid is used for the synthesis of substituted 1,2 and 1,3 optically active diols. Thus, diol I was prepared in 70% yield from II via the key intermediate acetonide III.

Synthetic Communications published new progress about Chiral synthons. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Name: (S)-Dimethyl 2-hydroxysuccinate.

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