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The coupling of aromatic moieties with saturated heterocyclic partners is currently an area of significant interest for the pharmaceutical industry. Herein, we present a procedure for the metal-free coupling of 4-, 5-, and 6-membered saturated heterocyclic p-methoxyphenyl (PMP) sulfonylhydrazones with aryl and heteroaromatic boronic acids. This procedure enables a simple, two-step synthesis of a range of functionalized sp2-sp3 linked bicyclic building blocks, including oxetanes, piperidines, and azetidines, from their parent ketones.

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

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Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for example Parkinson’s disease, Alzheimer’s disease and amyotrophic lateral sclerosis (ALS).

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

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Dual Gold-Catalyzed Three-Component Reaction: Efficient Synthesis of Indene-Fused Esters, Acids, and Lactones through Gold Vinylidene Intermediates

A dual gold(I)-catalyzed three-component reaction was developed to prepare indene-fused carboxylic acid derivatives from diynes, alcohols, and pyridine N-oxides in both inter- and intramolecular fashions. The pyridine N-oxides were found to exhibit distinct selectivity unlike the alpha-oxo gold carbene intermediates in the well-developed gold-catalyzed oxidative functionalization of alkynes. Experimental studies and DFT calculations support double nucleophilic substitution of a gold vinylidene intermediate.

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

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A bimetallic palladium(II) catalyzed synthesis of 1,2-dibromo compounds

A bimetallic palladium(II) catalyst containing a triketone ligand and a bridging dinitrogen ligand oxidizes aromatic and cyclic aliphatic olefins in bromide-containing aqueous-THF to 1,2-dibromo compounds and bromohydrins. With aromatic olefins, the 1,2-dibromo products were obtained in a 70-80% yield and the bromohydrins in a 10-15% yield; this observation is opposition to that obtained in chloride containing medium where the chlorohydrin product predominates. The oxidation of 2,3-dihydrofuran gave trans-2,3- dibromotetrahydrofuran, 3-oxotetrahydrofuran, and 3-bromo-2- hydroxytetrahydrofuran in relative yields of 75%, 15%, and 10%, respectively. On the other hand, the oxidation of cyclopentene and cyclohexene affords only trans-1,2-dibromo products in about 90% yield. The stereochemistry is consistent with an anti-at-tack of bromide followed by decomposition involving attack of bromide from the coordination sphere of the Pd(II). The procedure outlined here is a convenient method for the one step synthesis of 1,2-dibromides.

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

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ALKYNYL ALCOHOLS AND METHODS OF USE

The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over- activation of NF-kB signaling is observed.

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

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I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 22929-52-8, help many people in the next few years.category: Tetrahydrofurans

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2 Tyrosine kinase mediated signal transduction inhibitors (by machine translation)

[Problem] 2 tyrosine kinase mediated signal transduction inhibitor. (I) a pharmaceutically acceptable salt of the compound of the formula [a] and (In the formula, R1 , R2 , R3 , R4A , R4B , X1 , X2 , X3 , X4 , X5 And the n, as herein defined), pharmaceutical compositions containing the same, as well as preparation and use of the method, are disclosed herein. Figure 1 [drawing] (by machine translation)

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

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ESTROGEN RECEPTOR MODULATORS

Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.

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

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Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease

The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

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

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Biocatalytic Enantioselective Hydroaminations for Production of N-Cycloalkyl-Substituted L-Aspartic Acids Using Two C?N Lyases

N-cycloalkyl-substituted amino acids have wide-ranging applications in pharma- and nutraceutical fields. Here we report the asymmetric synthesis of various N-cycloalkyl-substituted l-aspartic acids using ethylenediamine-N,N?-disuccinic acid lyase (EDDS lyase) and a previously engineered variant of methylaspartate ammonia lyase (MAL-Q73A) as biocatalysts. Particularly, EDDS lyase shows broad non-natural substrate promiscuity and excellent enantioselectivity, allowing the selective addition of homo- and heterocycloalkyl amines (comprising four-, five- and six-membered rings) to fumarate, giving the corresponding N-cycloalkyl-substituted l-aspartic acids with >99% e.e. This biocatalytic methodology offers an alternative synthetic choice to prepare difficult N-cycloalkyl-substituted amino acids. Given its very broad amine scope, EDDS lyase is an exceptionally powerful synthetic tool that nicely complements the rapidly expanding toolbox of biocatalysts for asymmetric synthesis of noncanonical amino acids. (Figure presented.).

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

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gamma-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration

An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. gamma-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.

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