- Method for selectively oxidizing cumene compounds
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The invention relates to a method for selectively oxidizing cumene compounds, and the method comprises the following steps: placing cumene compounds shown in a formula (I), an iron porphyrin catalyst,an oxidant and a dispersant into a ball milling tank, sealing the ball milling tank, performing ball milling for 3 to 24 hours at a rotating speed of 100 to 800 rpm at room temperature, stopping ballmilling once every 1 to 3 hours in the ball milling process, discharging gases in the ball milling tank, finishing the reaction, and performing post-treatment on a reaction mixture to obtain product2-phenyl-2-propanol compound shown in a formula (II); according to the invention, the oxidation conversion of the cumene and derivatives thereof is realized through solid-phase ball milling, the reaction mode is novel, the operation is convenient, and the energy consumption is low; the method needs no organic solvent, thus effectively avoiding the use of toxic and harmful organic solvents and being green and environment-friendly; has low peroxide content and high safety factor, and high 2-phenyl-2-propanol and derivative selectivity and meets the social requirements of the current green chemical process, environmental compatibility chemical process and biological compatibility chemical process.
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Paragraph 0113; 0114
(2019/11/21)
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- LXR AGONISTS AND USES THEREOF
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This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.
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Paragraph 0348; 0349
(2017/03/28)
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- LXR AGONISTS AND USES THEREOF
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This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.
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Page/Page column 65
(2015/07/23)
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- Access to "friedel-Crafts-Restricted" tert -alkyl aromatics by activation/methylation of tertiary benzylic alcohols
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Herein we describe a two-step protocol to prepare m-tert-alkylbenzenes. The appropriate tertiary benzylic alcohols are activated with SOCl2 or concentrated HCl and then treated with trimethylaluminum, affording the desired products in 68-97% yields (22 examples). This reaction sequence is successful in the presence of a variety of functional groups, including acid-sensitive and Lewis-basic groups. In addition to t-Bu groups, 1,1-dimethylpropyl and 1-ethyl-1-methylpropyl groups can also be installed using this method.
- Hartsel, Joshua A.,Craft, Derek T.,Chen, Qiao-Hong,Ma, Ming,Carlier, Paul R.
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experimental part
p. 3127 - 3133
(2012/05/20)
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- VITAMIN D RECEPTOR AGONISTS AND USES THEREOF
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Disclosed is a compound of Formula (I), in which R1, R2, R3, R4, R5, R6, X, and a are defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition comprising a compound or salt therof of Formula (I) and a method of treating a disease which benefits from the modulation of the vitamin D receptor, such as a bone disorder, cardiovascular disease, a cardiovascular complication associated with renal disease, endothelial dysfunction, hyperparathyroidism, hypocalcemia, an immune disorder, left ventricular hypertrophy, a proliferative disease, proteinuria, renal disease, and thrombosis.
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Page/Page column 86-87
(2010/11/04)
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- Vitamin D analogues
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The invention relates to compounds of formula I STR1 in which formula X is hydrogen or hydroxy; Y is oxygen, sulphur, or oxidized sulfur (S(O) or S(O2)); R1 and R2, which may be the same or different, stand for hydrogen or C1 -C6 hydrocarbyl, or R1 and R2, taken together with the carbon atom (starred in formula I) bearing the group X, form a C3 -C8 carbocyclic ring; Q is a C1 -C8 hydrocarbylene diradical. R3 is hydrogen or C1 -C6 hydrocarbyl. R1, R2 and/or Q, may be optionally substituted with one or more deuterium or fluorine atoms; n is 0 or 1. The present compounds show antiinflammatory and immunomodulating effects as well as a strong activity in inducing cell differentiation and inhibiting undesirable proliferation of certain cancer and skin cells.
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- A rapid method for preparing chromogenic alfa-amylase substrate compounds at high preparative yields
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A method for preparing chromogenic α-amylase substrate compounds at substantially high preparative yields in a relatively short period of time by the transglucosylation of a chromogenic glucoside compound to a maltooligosaccharide chain. The concentration of the maltooligosaccharide compound is greater than about 3 times the concentration of the chromogenic glucoside compound to result in at least about 50% of the chromogenic glucoside compound being converted to the desired chromogenic α-amylase substrate compound.
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- Chromogenic acridinone enzyme substrates
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Chromogenic acridinone enzyme substrate compounds comprising 7-hydroxy-9H-acridin-2-one chromogens derivatized at the 7-hydroxy-position with an enzymatically-cleavable group and disubstituted at the 9-position with alkyl or aryl groups, which can be the same or different, preferably lower alkyl or phenyl, respectively, or together form a cyclohexa-2,5-diene-4-one residue or a 4-hydroxycycloxhexyl residue, and 7-hydroxy-1,3-dihalo-9,9-dimethyl-acridin-2-one intermediates useful for the preparation of the novel chromogenic acridinone enzyme substrate compounds and methods therefor. The enzymatically-cleavable group is a radical of a compound Y-OH comprising an enzyme-specific moiety which is capable of being cleaved by a specific enzyme wherein a deprotonated form of the chromogen is liberated having an absorbance maximum in basic solution which is substantially greater than the absorbance maximum of the chromogenic acridinone enzyme substrate compound to provide a distinct change in absorbance which can be accurately measured and correlated to the amount of enzyme present in a liquid test sample.
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- Process for preparation of hydroxyaryldialkylcarbinols
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The preparation of hydroxyaryldialkylcarbinols by the reaction of hydroxyaryl alkyl ketones or alkyl hydroxyarenecarboxylates with Grignard reagents in a mixed ether-aromatic hydrocarbon solvent is frequently difficult on a large-scale basis because of formation of a voluminous precipitate of mixed magnesium salt. In an improvement in this process, a solution of the ketone or ester in an ether is added to the solution of the Grignard reagent.
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