Discovery of (R)-4-Benzyl-2-oxazolidinone

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Enantioselective Synthesis of a (+)-(2R, 3R)-1,4-Benzodioxane-7-carbaldehyde Derivative, a Key Intermediate in the Total Synthesis of Haedoxan Analogs

(+)-(2R, 3R)-7-Formyl-6-methoxy-2-methoxymethyl-3-(3,4-methylenedioxyphenyl)-2,3-dihydro- 1,4-benzodioxin (2), a key building block for the total synthesis of haedoxan A, was synthesized from (4R)-4-(phenylmethyl)-2-oxazolidinone (3) in ten steps with a 12% overall yield.

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The Absolute Best Science Experiment for (R)-4-Benzyl-2-oxazolidinone

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Total synthesis of (+)-lysergic acid

A total synthesis of (+)-lysergic acid, which features the C-C bond formation between C10 and C11 via cleavage of an aziridine ring, was accomplished.

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The stereoselective total synthesis of PF1163A

A stereoselective total synthesis of 13-membered macrocycle PF1163A, an antifungal agent, has been accomplished for the first time starting from d-xylose. This approach involves a diastereoselective allylation of lactal ether,3a reductive ring opening of tetrahydrofuran ring,3b asymmetric methylation reaction, Yamaguchi esterification, and ring closing metathesis as key steps.

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Extended knowledge of (R)-4-Benzyl-2-oxazolidinone

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A convergent synthesis of the C1-C16 segment of goniodomin A via palladium-catalyzed organostannane-thioester coupling

A convergent synthesis of the C1-C16 segment of goniodomin A, an actin-targeting marine polyether macrolide natural product, has been achieved via a 2-fold application of palladium-catalyzed organostannane-thioester coupling.(Figure Presented)

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Asymmetric synthesis of non-natural homologues of lysine

A series of non-natural amino acid homologues of L- and D-lysine have been synthesized and protected for use in solid-phase peptide synthesis. With these residues, electrostatics and hydrophobicity of peptides can be enhanced or altered.

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The important role of (R)-4-Benzyl-2-oxazolidinone

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NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

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Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 1: Synthetic Strategy and Preparation of a Common Precursor

The synthetic strategy for producing multigram quantities of (+)-discodermolide (1) using a hybridized Novartis-Smith-Paterson synthetic route via common precursor 3 is described. In the first part of this five-part series, we present a multikilogram preparation of alpha-methyl aldehyde 10 from Roche ester, its syn-aldol reaction with Evans boron enolate, removal of the chiral auxiliary, and the preparation of Weinreb amide 3 (Smith common precursor). The common precursor was produced without any chromatography.

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Brief introduction of 102029-44-7

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Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: Preparation of (2S,3R)-3-(3,4- difluorophenyl)-2-(4-fluorophenyl)-4-hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement

Novel benzodiazepine-containing gamma-secretase inhibitors for potential use in Alzheimer’s disease have been designed that incorporate a substituted hydrocinnamide C-3 side chain. A syn combination of alpha-alkyl or aryl and beta-hydroxy or hydroxymethyl substituents was shown to give highly potent compounds. In particular, (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4-hydroxy- N-((3S)-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)butyramide (34) demonstrated excellent in vitro potency (IC50 = 0.06nM). 34 could also be selectively methylated to give [3H]-28, which is of use in radioligand binding assays.

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New explortion of 102029-44-7

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A medicine intermediate N – Boc – trans -4 – methyl – L – proline methyl ester preparation method (by machine translation)

The invention discloses a N – Boc – trans – 4 – methyl – L – proline methyl ester preparation method, compound D – glutamic acid in the diazotization reaction, esterification reaction, hydrolysis to obtain compound 16; compound 16 with TBSCl reaction to obtain compound 17; compound 17 hydrolysis, then with the (R)- 4 – benzyl – 2 – oxazolidinone reaction to obtain compound 18; compound 18 undergo the substitution reaction to obtain compound 19; compound 19 reduction to obtain compound 20, then with the DPPA, DBU reaction, to obtain the compound 21; compound 21 deprotection to obtain compound 22; compound 22 dehydroxylated, and then dissolved in methanol in the reaction under the condition of iodine potassium hydroxide to obtain compound 23; compound 23 deprotected after reaction with P-toluene sulfonyl chloride, to obtain compound 24; compound 24 in the catalytic reaction under the condition of the ring, adding alkaline substance and Boc anhydride reaction to obtain compound 4. Preparation method of the invention overcomes the existing technology in the preparation N – Boc – 4 – methyl proline methyl ester exists when the defect of the stereo selectivity is not good, the use of a readily available and inexpensive starting materials, to improve the yield of the process. (by machine translation)

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Extracurricular laboratory:new discovery of 102029-44-7

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BIPHENYL CARBOXYLIC ACIDS AND DERIVATIVES THEREOF

The present invention relates to compounds having the general Formula (I) with the definitions of R1, R2, R3, and R4 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer”s disease and their use for the modulation of gamma-secretase activity.

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