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PROBLEM TO BE SOLVED: […] choresterol lowering manufacturing method. SOLUTION: intermediate protecting group (M1) is generated by production of […] (I). [R 1 is benzyl group such as, R 2 protective group or the like, the protective groups of etherifying silyl ether. ] Selected drawing: no (by machine translation)

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Reference:
Oxazolidine – Wikipedia,
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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, 189028-95-3, name is (S)-3-((S)-5-(4-Fluorophenyl)-5-hydroxypentanoyl)-4-phenyloxazolidin-2-one, introducing its new discovery. Product Details of 189028-95-3

The S alcohol in the benzylic position of compound 2, a key feature of a novel cholesterol lowering agent Ezetimibe, was introduced by the (R)-MeCBS catalyzed asymmetric carbonyl reduction of ketone 1 using borane tetrahydrofuran complex (BTHF) as the reducing agent. The chemo- and enantioselectivity was dramatically enhanced by using an acid as a scavenger of the stabilizer sodium borohydride present in the commercially supplied pure BTHF. The effect of the critical reaction parameters such as addition mode of reagent, temperature, acids as well as water content on the selectivity has been examined. This reaction has been successfully applied in the commercial process for the preparation of the key intermediate 2 for Ezetimibe.

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Reference of 189028-95-3, 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.189028-95-3, Name is (S)-3-((S)-5-(4-Fluorophenyl)-5-hydroxypentanoyl)-4-phenyloxazolidin-2-one, molecular formula is C20H20FNO4. In a article,once mentioned of 189028-95-3

The present invention relates to a new method for preparing ezetimibe comprising a step of cyclizing the compound (4S)-phenyl-3-[(5S)-(4-fluorophenyl)-(2R)-[(1S)-(4-fluorophenylamino)-1-(4-nitrophenyl)methyl]-5-hydroxypentanoyl]oxazolidin-2-one or the derivatives thereof in which the hydroxyl group is protected. The invention also relates to new intermediates used in this method.

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The application discloses one intermediate folds Mai Bu 3 – [(2R, 5S) – 5 – (4-fluoro phenyl) – 2 – [(S) – [(4-fluoro phenyl (amino)]] [4-R 1 oxy] phenyl] methyl] – 1-oxo-5 – [( trimethyl silicon ) oxy] phenyl] – 4-phenyl-(4S) – 2-oxazolidinone catalytic synthesis method, by adopting the AlCl 3/SiO 2 catalyst or SO 42-/TiO 2 solid acid catalyst to replace the original titanium tetrachloride and isopropyl alcohol titanium catalyst, reduces the environmental pollution and to the requirements of the production equipment, solves the problem of separation and recovery of the catalyst, the scale continuous production of mai Buaccording to booklet become possible. (by machine translation)

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Product Details of 189028-95-3, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 189028-95-3, name is (S)-3-((S)-5-(4-Fluorophenyl)-5-hydroxypentanoyl)-4-phenyloxazolidin-2-one. In an article,Which mentioned a new discovery about 189028-95-3

3H-Sch 58235 was prepared at a specific activity of 29.1 Ci/mmol by Ir(COD)(Cy3P)PyPF6 catalysed exchange with tritium gas. 14C-Sch 58235 was prepared in three steps from p-hydroxy[ring-U-14C]benzaldehyde with an overall radiochemical yield of 21%. 13C6-Sch 58235 was similarly prepared in three steps from p-hydroxy[ring-U-13C6]benzaldehyde in an overall yield of 41%. Copyright

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The invention of the formula (VI) compound and its preparation method, the compound of formula (VI) and an intermediate type (V) compound of formula and its preparation method, the method does not need the use of silyl protecting agent can yield compounds of formula (V), by the formula (VI) can further compound, further preparation according to folds Mai Bu, thus simplifying the operation, and is suitable for industrial production, (by machine translation)

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Application of 189028-95-3, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 189028-95-3, (S)-3-((S)-5-(4-Fluorophenyl)-5-hydroxypentanoyl)-4-phenyloxazolidin-2-one, introducing its new discovery.

Low temperature NMR studies revealed that a diastereoselective Mannich reaction between a phenyl oxazolidone-derived titanium enolate and an aromatic aldimine was found to occur only after introduction of a proton source. While various protic additives could be used to promote the transformation, the best results were obtained using AcOH to afford the corresponding Mannich products in high diastereoselectivities and yields.

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The application discloses one intermediate folds Mai Bu 3 – [(2R, 5S) – 5 – (4-fluoro phenyl) – 2 – [(S) – [(4-fluoro phenyl (amino)]] [4-R 1 oxy] phenyl] methyl] – 1-oxo-5 – [( trimethyl silicon ) oxy] phenyl] – 4-phenyl-(4S) – 2-oxazolidinone synthesis method, through the use of solid H-ZSM-5 molecular sieve catalyst and/or Co-ZSM-5 molecular sieve catalyst to replace the original titanium tetrachloride and isopropyl alcohol titanium catalyst, reduces the environmental pollution and to the requirements of the production equipment, solves the problem of separation and recovery of the catalyst, the continuous production of mai Buaccording to booklet laid the foundation for a large scale. (by machine translation)

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The invention discloses a according to the method for synthesizing intermediate folds mai bu, comprises the following steps: in under the nitrogen atmosphere, of formula (2) compound are added to in tetrahydrofuran to obtain solution A, A the solution temperature to 5 C to 10 C, and to the solution of (-) – A dropping two different pine pinane base chlorine borane, stirring the reaction, after the reaction is finished to obtain solution B, the solution B cooling to – 20 C to 0 C, aqueous solution of […], adjusting solution B of pH=5 – 8, the ethyl acetate extract adjusting pH of the solution B, evaporate ethyl acetate to obtain the residue C, to the remainder of the organic solvent is added in the C, standing, pouring the organic solvent, the residue obtained D, D to the residue in toluene is added to obtain solution E, heating and stirring solution after E, natural cooling, the solution is put into the freezing environment in E, filtering, drying formula (1) compound of the solid, the method is simple and easy, and the cost is low. The reaction is shown as follows: (by machine translation)

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PROBLEM TO BE SOLVED: […] choresterol lowering manufacturing method. SOLUTION: intermediate protecting group (M1) is generated by production of […] (I). [R 1 is benzyl group such as, R 2 protective group or the like, the protective groups of etherifying silyl ether. ] Selected drawing: no (by machine translation)

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Reference:
Oxazolidine – Wikipedia,
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