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“ONE-POT” SYNTHESIS OF DISYMMETRICALLY alpha,alpha’-DISUBSTITUTED SUCCINIC ANHYDRIDES PRECURSORS

A “one-pot” synthesis for disymmetrically alpha,alpha’-disubstituted succinic anhydrides precursors isreported in the present paper.Substituents are aryl, primary or secondary alkyl groups.This reaction represents a simple and quick method with fair yields.

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

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Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes

Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.

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

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Controlled drug release: New water-soluble prodrugs of an HIV protease inhibitor

We designed and synthesized a series of highly water-soluble prodrugs of an HIV protease inhibitor, KNI-727 (1), containing tandem-linked two auxiliary units, a solubilizing moiety and a self-cleavable spacer. Prodrugs with an ionized amino group at the solubilizing moiety exhibited a remarkable increase of water-solubility (>104 fold) compared to the parent drug 1. These prodrugs released 1 not enzymatically, but chemically via an intramolecular cyclization-elimination reaction through an imide formation in physiological conditions. Diversified rates of parent drug release were observed when the chemical structure of both the solubilizing and the spacer moieties were modified. This new approach for water-soluble prodrugs will enable to control chemically the release of parent drug as well as to maintain high water-solubility.

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

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Anti-AIDS agents. 48. Anti-HIV activity of moronic acid derivatives and the new melliferone-related triterpenoid isolated from Brazilian propolis

A new triterpenoid named melliferone (1), three known triterpenoid, moronic acid (2), anwuweizonic acid (3), and betulonic acid (4), and four known aromatic compounds (5-8) were isolated from Brazilian propolis and tested for anti-HIV activity in H9 lymphocytes. Moronic acid (2) showed significant anti-HIV activity (EC50 < 0,1 mug/mL, TI > 186) and was modified to develop more potent anti-AIDS agents.

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

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The pseudopeptide pyrrolidinedione natural products moiramide B and andrimid represent a new class of antibiotics that target bacterial fatty acid biosynthesis. Structure-activity relationship (SAR) studies revealed a high degree of variability for the fatty acid side chain, allowing optimization of physicochemical parameters, and a restricted SAR for the pyrrolidinedione group, indicating major relevance of this subunit for efficient target binding.

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

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The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X¿ and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases

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

Brief introduction of 2,2-Dimethylsuccinicanhydride

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An efficient synthesis of low-covered polyrotaxanes grafted with poly(epsilon-caprolactone) and the mechanical properties of its cross-linked elastomers

Advanced polyrotaxane elastomers were fabricated by the synthesis of poly(epsilon-caprolactone)-grafted polyrotaxanes with significantly lower coverage than previously achieved. The time course for the complexation of alpha-cyclodextrin with an end-functionalized polyethylene glycol (PEG) was analyzed by subsequent end-capping and polyrotaxane isolation, which revealed that the bulkiness of the PEG end group affects the time required for complex nucleation and the resulting coverage. Low-coverage poly(epsilon-caprolactone)-grafted polyrotaxanes were synthesized in a facile and large-scale manner by optimizing the simultaneous hydrolysis of the end-capping groups and the solubility of the product during the ring-opening polymerization of epsilon-caprolactone. Cross-linking the thermoplastic graft polyrotaxanes yielded elastomers that are much more extensible than conventional elastomers with fivefold higher coverages. Elastomers with lower coverages behave as ideal elastic bodies due to chain sliding through the cross-links, which suggests that the arrangement entropy of the cyclic components, which counteracts chain sliding, is substantially decreased by reduced coverage.

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

Discovery of 2,2-Dimethylsuccinicanhydride

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PYRIDAZINONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS

Compounds of formula (1) are effective PDE4 inhibitors in which R1 is 1-4C-alkyl and R2 is 1-4C-alkyl, R3 represents a phenyl dervative of formulae (a) or (b) wherein R4 is 1-4C-alkoxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R5 is 1-8C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R6 is 1-4C-alkoxy, 3-5C-cycloalkoxy, 3-5C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R7 is 1-4C-alkyl and R8 is hydrogen or 1-4C-alkyl, or wherein R7 and R8 together and with inclusion of the two carbon atoms, to which they are bonded, form a spiro-linked 5-, 6-or 7-membered hydrocarbon ring, optionally interrupted by an oxygen or sulphur atom and R9 is hydroxyl, halogen, nitro, cyano, 1-4C-alkyl, trifluoromethyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, hydroxycarbonyl, hydroxycarbonyl-1-4C-alkyl, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonyl, benzyloxy,-C(O)R10,-S(O)2-R11,-O(CH2)n-C(O)-R12,-(CH2),-C(O)-R26 or-N(R29)R30.

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

Brief introduction of 2,2-Dimethylsuccinicanhydride

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Reference of 17347-61-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.17347-61-4, Name is 2,2-Dimethylsuccinicanhydride, molecular formula is C6H8O3. In a Patent£¬once mentioned of 17347-61-4

3,28-DISUBSTITUTED BETULINIC ACID DERIVATIVES AS ANTI-HIV AGENTS

The present invention provides compounds of Formula (I) and Formula (II): along with compositions containing the same and methods of use thereof in treating viral infections such as HIV infections.

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

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Preparation of tertiary alcohols and gamma-lactones from allylsilanes and anhydrides

The TiCl4-mediated reaction of allyltrimethylsilane and anhydrides yields alkyldiallylcarbinols.In the case of the diallylsilane 1,8-bis(trimethylsilyl)octa-2,6-diene and cyclic anhydrides, spiro-lactones resulting from a gem-diallylation are obtained with high stereoselectivity. allylsilane / anhydride / dialkylation

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