Archives for Chemistry Experiments of (4S,5R)-4-Methyl-5-phenyloxazolidin-2-one

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Methods are disclosed to treat or prevent at least one disease or condition in a subject in need thereof comprising administering a compound of Formula (I): (I) or a pharmaceutically acceptable salt, or ester thereof, wherein R1 and R2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C1 -C6 alkyl groups, with the proviso that R1 and R2 are not both hydrogen or a pharmaceutically acceptable salt or ester thereof. Such diseases or conditions may relate to coronary heart disease (CHD), for example atherosclerosis; metabolic syndrome/insulin resistance; and/or a dyslipidemic condition such as hypertriglyceridemia (HTG), elevated LDL- cholesterol, elevated total-cholesterol, elevated Apo B and low HDL-cholesterol. The present disclosure further provides for a method of reducing atherosclerosis development. Pharmaceutical compositions comprising a compound of Formula (I) are also disclosed.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H2116NO – PubChem

 

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The present invention relates to an improved process for the preparation of renin inhibitor Aliskiren intermediates of Formula-II and further conversion into Aliskiren and its pharmaceutically acceptable salts.

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All the stereoisomers of butanol type 1,7-seco-2,7?-cyclolignane were stereoselectively synthesized by employing (S)- and (R)-Evans’ auxiliaries to construct the stereochemistry. (+)- and (-)-Kadangustin J and their diastereomers were also prepared. The optical purity of the synthesized butanol type 1,7-seco-2,7?-cyclolignane was more than 99%ee.

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The preparation of a series of new fumagillin-derived MetAP-2 inhibitors is described. The synthetic approach was designed so as to permit modification of the fumagillin backbone at sites inaccessible through semisynthesis or previously existing total syntheses. An Evans aldolization and a ring-closing metathesis allowed the preparation of a pivotal intermediate which could then be functionalized in various ways using already established or newly developed methodologies.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: (R)-4-Benzyl-2-oxazolidinone, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 102029-44-7, Name is (R)-4-Benzyl-2-oxazolidinone, molecular formula is C10H11NO2

A stereoselective synthesis of the complete C1-C16 framework of tianchimycins A and B is described. Key transformations include Horner-Wadsworth-Emmons, Evans aldol, Gilman’s and stereoselective alkylation reactions.

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To identify novel antitrypanosomal agents based on Janadolide, a potent macrocyclic polyketide-peptide hybrid, a macrolactonization strategy was explored. We prepared des-tert-butyl Janadolide and evaluated its antitrypanosomal activity. Our findings suggest that the tert-butyl group is necessary for the desired bioactivity.

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The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor alpha (PPARalpha), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride). It relates to substituted phenylpropanoic acid derivatives represented by a general formula (1), their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

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This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an trans-azetidinone represented by the formula STR1 from a carboxylic acid R2 -D-CH2 -COOH, an aldehyde R1 -A-CHO and an amine RNH2, by the steps of: (a1) converting a carboxylic acid to the corresponding acid chloride; (b1) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a1); (c1) enolizing the product of step (b1) and condensing with the aldehyde; (d1) hydrolyzing the product of step (c1); (e1) condensing the product of step (d1) with the amine; and (f1) cyclizing the product of step (e1). Alternatively, the process comprises (a2) enolizing the product of step (b1) and condensing, in the presence of a Lewis acid, with a Schiff’s base prepared from the aldehyde and the amine; and (b2) cyclizing the product of step (a2).

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(Chemical Equation Presented) The key fragment (2a or 2b) in a total synthesis of the cytotoxic macrolide (-)-amphidinolide K (1) has been achieved from synthons C9-C14 (3) and C15-C22 (4), which have both been prepared from glutamic acid in good overall yields.

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Oxazolidine – Wikipedia,
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Archives for Chemistry Experiments of (R)-4-Benzyl-2-oxazolidinone

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Histone deacetylase (HDAC) proteins are epigenetic regulators that deacetylate protein substrates, leading to subsequent changes in cell function. HDAC proteins are implicated in cancers, and several HDAC inhibitors have been approved by the FDA as anticancer drugs, including SAHA (suberoylanilide hydroxamic acid; Vorinostat and Zolinza). Unfortunately, SAHA inhibits most HDAC isoforms, which limits its use as a pharmacological tool and may lead to side effects in the clinic. In this work SAHA analogues substituted at the C2 position were synthesized and screened for HDAC isoform selectivity in vitro and in cells. The most potent and selective compound, C2-n-hexyl SAHA, displayed submicromolar potency with 49- to 300-fold selectivity for HDAC6 and HDAC8 compared to HDAC1, -2, and -3. Docking studies provided a structural rationale for selectivity. Modification of the nonselective inhibitor SAHA generated HDAC6/HDAC8 dual selective inhibitors, which can be useful lead compounds toward developing pharmacological tools and more effective anticancer drugs.

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