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PROCESS FOR THE PREPARATION OF A CHIRAL BETA AMINOACID DERIVATIVE AND INTERMEDIATES THEREOF

It comprises a process for the preparation of sitagliptin, or its pharmaceutically acceptable salts, or its solvates, including hydrates, comprising: a) coupling an halo-2,4,5-trifluorobenzene with a compound of formula (IV) to give N-protected sitagliptin; the coupling being carried out via the formation of an organocupric compound of the halo-2,4,5-trifluorobenzene or, alternatively, via the formation of a organozinc compound of a compound of formula (IV); where R1 is hydrogen or an amino protective group; R2 is an amino protective group; or alternatively R1 and R2 taken together form a phtalimido group; X is Br or I; and Y is Br, I or R3SO3- wherein R3 is (C1-C4)- alkyl, phenyl, or phenyl mono- or disubstituted by a (C1-C4)-alkyl radical; b) submitting the N-protected sitagliptin to a deprotection reaction; and c) optionally its conversion into a pharmaceutically acceptable salt. It also comprises new intermediate compounds useful in such preparation process.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 87219-29-2, name is (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate, introducing its new discovery. Recommanded Product: (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate

Synthesis of 3-Methoxy-2-iso-oxacephalosporin

Optically active 3-methoxy-2-iso-oxacephalosporins are efficiently prepared via intramolecular acylation as a key step.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 87219-29-2 is helpful to your research. Application of 87219-29-2

Application of 87219-29-2, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 87219-29-2, molcular formula is C12H13NO4, introducing its new discovery.

Diamine derivatives

A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group 1 in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger’s disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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A versatile synthetic route to indolizidines, (+)-7-deoxy-6- epicastanospermine, (-)-7,8-dideoxy-6-epicastanospermine and (-)-N- acetylslaframine

(+)-7-Deoxy-6-epicastanospermine 1, (-)-7,8-dideoxy-6- epicastanospermine 2 and (-)-N-acetylslaframine 4 have been synthesized via the stereoselective intramolecular iodocyclization of trichloroacetimidates generated from cis-olefinic allylic alcohols 7 and 15, respectively.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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The invention relates to compounds having the formula: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical compositions, kits and articles of manufacture comprise the compounds.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Electric Literature of 87219-29-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.87219-29-2, Name is (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate, molecular formula is C12H13NO4. In a article,once mentioned of 87219-29-2

3-D-QSAR of N-substituted 4-amino-3,3-dialkyl-2(3H)-furanone GABA receptor modulators using molecular field analysis and receptor surface modelling study

We report the theoretical validation of the experimentally observed structure-activity relationships (SAR) of a set of N-substituted 4-amino-3,3-dialkyl-2(3H)-furanone GABA receptor modulators showing positive allosteric modulatory activity of the GABAA receptor similar to that shown by Loreclazole. Efforts were made to explain some of the conclusions drawn during this study based on a solitary instance of occurrence of the observation within the dataset. Some of the conclusions selected for study included (i) the enhanced activity for the R enantiomer of a compound, (ii) enhanced activity for a compound with an amide type functionality vis-a-vis an amine type functionality at C-4, (iii) enhanced activity for a compound with a carboxamide or carbamate type functionality linking the end group at C-4 over a compound with only the end group attached, provided the alkyl groups attached at C-3 are identical in both cases. The 3-D-QSAR method of molecular field analysis along with receptor-ligand complex stability studies were found to be the most suitable for explaining these activities. While the first conclusion was comprehensively proven, significant support was obtained in case of the latter two. Further comprehensive study is underway and we hope to report them shortly.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Baeyer?Villiger monooxygenase-catalyzed desymmetrizations of cyclobutanones. Application to the synthesis of valuable spirolactones

A series of gamma-butyrolactone derivatives, including some spiranic ones, was obtained through desymmetrization of the corresponding prochiral 3-substituted cyclobutanones via Baeyer?Villiger monooxygenase (BVMO)-catalyzed oxidation. After reaction optimization using several commercial enzymes, both antipodes of various lactones were synthesized in most cases with >90% conversion and >80% enantiomeric excess under mild reaction conditions. In some cases alcohol formation was also observed (up to 40% conversion) as an undesired side reaction due to the presence of alcohol dehydrogenases in these preparations. Selected transformations were achieved on a 100 mg scale showing the possibilities of these oxidative biocatalysts as a new source of highly interesting compounds.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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NOVEL BETA-LACTAM COMPOUNDS AND PROECSS FOR PRODUCING THE SAME

1. A beta-lactam compound of the formula [1]; ???wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, -C(R3)=NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 87219-29-2, Name is (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate, molecular formula is C12H13NO4

Studies towards the total synthesis of batzelladine A

Application of a diastereoselective three-component coupling to the bicyclic core of the batzelladine alkaloids is described. The synthesis features the elaboration of glutamic acid by use of Eschenmoser sulfide contraction. An earlier approach is also included, which shows some limitations of dithiane chemistry when applied to the particular compounds required for this target.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 87219-29-2, in my other articles.

Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Synthetic Route of 87219-29-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.87219-29-2, Name is (S)-Benzyl (5-oxotetrahydrofuran-3-yl)carbamate, molecular formula is C12H13NO4. In a Article£¬once mentioned of 87219-29-2

Discovery of Macrocyclic Inhibitors of Apurinic/Apyrimidinic Endonuclease 1

Apurinic/apyrimidinic endonuclease 1 (APE1) is an essential base excision repair enzyme that is upregulated in a number of cancers, contributes to resistance of tumors treated with DNA-alkylating or -oxidizing agents, and has recently been identified as an important therapeutic target. In this work, we identified hot spots for binding of small organic molecules experimentally in high resolution crystal structures of APE1 and computationally through the use of FTMAP analysis (http://ftmap.bu.edu/). Guided by these hot spots, a library of drug-like macrocycles was docked and then screened for inhibition of APE1 endonuclease activity. In an iterative process, hot-spot-guided docking, characterization of inhibition of APE1 endonuclease, and cytotoxicity of cancer cells were used to design next generation macrocycles. To assess target selectivity in cells, selected macrocycles were analyzed for modulation of DNA damage. Taken together, our studies suggest that macrocycles represent a promising class of compounds for inhibition of APE1 in cancer cells.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem