- methyl-2,2-bis(4-hydroxyphenyl)methyl acetate synthesis method
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The present invention relates to the field of production of chemical industry products, particularly to a methyl-2,2-bis(4-hydroxyphenyl)methyl acetate synthesis method. According to the synthesis method, phenol and glyoxylic acid are adopted as main raw materials, and a condensation and esterification two-step process route is performed; in the condensation reaction step, phenol, water and glyoxylic acid are firstly added at a low temperature condition and then concentrated sulfuric acid is added in a dropwise manner, or glyoxylic acid and water are firstly added and then phenol and concentrated sulfuric acid are simultaneously added in a dropwise manner, or phenol and water are firstly added and then glyoxylic acid and concentrated sulfuric acid are simultaneously added in a dropwise manner; and the filter cake obtained through the condensation reaction is added with methanol and concentrated sulfuric acid, a heating reflux esterification reaction is performed, concentration and filtration are performed to obtain a crude product, the crude product is dried, and the dried crude product is subjected to recrystallization purification to obtain the methyl-2,2-bis(4-hydroxyphenyl)methyl acetate. According to the present invention, the extraction with a large amount of the organic solvent is avoided, the operation is simple, the pollution is low, the yield is high, and the synthesis method is suitable for large-scale industrial production.
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Paragraph 0025-0027
(2017/08/31)
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- Symmetrical bis(heteroarylmethoxyphenyl)alkylcarboxylic acids as inhibitors of leukotriene biosynthesis
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Symmetrical bis(quinolylmethoxyphenyl)alkylcarboxylic acids were investigated as inhibitors of leukotriene biosynthesis and 4,4-bis(4-(2-quinolylmethoxy)phenyl)pentanoic acid sodium salt (47·Na) met our design parameters for a drug candidate (ABT-080). This compound was readily synthesized in three steps from commercially available diphenolic acid. Against intact human neutrophils, 47·Na inhibited ionophore-stimulated LTB4 formation with an IC50 = 20 nM. In zymosan-stimulated mouse peritoneal macrophages producing both LTC4 and PGE2, 47·Na showed 9000-fold selectivity for inhibition of LTC4 (IC50 = 0.16 nM) over PGE2 (IC50 = 1500 nM). Preliminary pharmacokinetic evaluation in rat and cynomolgus monkey demonstrated good oral bioavailability and elimination half-lives of 9 and 5 h, respectively. Pharmacological evaluation of leukotriene inhibition with oral dosing was demonstrated in a rat pleural inflammation model (ED50 = 3 mg/kg) and a rat peritoneal passive anaphylaxis model (LTB4, ED50 = 2.5 mg/kg; LTE4, ED50 = 1.0 mg/kg). In a model of airway constriction induced by antigen challenge in actively sensitized guinea pigs, 47·Na dosed orally blocked bronchoconstriction with an ED50 = 0.4 mg/kg, the most potent activity we have observed for any leukotriene inhibitor in this model. The mode of inhibitory action of 47·Na occurs at the stage of 5-lipoxygenase biosynthesis as it blocks both leukotriene pathways leading to LTB4 and LTC4 but not PGH2 biosynthesis. However, 47·Na does not inhibit 5-lipoxygenase catalysis in a broken cell enzyme assay; therefore it is likely that 47·Na acts as a FLAP inhibitor.
- Kolasa,Gunn,Bhatia,Basha,Craig,Stewart,Bouska,Harris,Hulkower,Malo,Bell,Carter,Brooks
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p. 3322 - 3334
(2007/10/03)
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- Salicylic acid derivatives
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The heat-sensitive recording material disclosed comprises a colorless or pale colored dyestuff precursor, one or more salicylic acid derivative of the formula (1) or metal salt of the derivative and an aliphatic amide compound having 18?60 carbon atoms in molecular structure, and is excellent in thermal response and preservation stability of white portions and images. STR1 wherein X1 and X2 are a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an aralkyl group or an aryl group, Y1 and Y2 are an oxygen atom or a sulfur atom, R1 is a hydrogen atom, an alkyl group, an aralkyl group or an aryl group, and R2 is an alkyl group, an alkenyl group, an aralkyl group or an aryl group.
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