专利号:US-6995289-B2 优先权日:2000-08-02 标题 :Process for synthesis of alpha, beta-unsaturated ketones 发明人:PATEL IAN; HOPES PHILIP 权利人:ASTRAZENECA AB 摘要:A method for the synthesis of an α,β-unsaturated ketone useful for making substituted 1,4-dihydropyridines is described by reacting an aldehyde with pyrrolidine and then adding a ketone followed by trifluoroacetic acid at low temperature. The synthesis is used in a process for making substituted 1,4-dihydropyridines wherein a vinylogous amide is prepared by reacting a 1,3-cyclohexanedione with a phenylethylamine. The α,β-unsaturated ketone can be reacted with a vinylogous amide to form a 1,5-diketone which can be converted to a substituted 1,4-dihydropyridine.
专利号:US-2009264680-A1 优先权日:2004-07-07 标题:Process for the synthesis and purification of (4-methoxybutyl) (4-trifluoromethylphenyl) methanone 发明人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 权利人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 摘要:A process for the preparation of 4-trifluoromethylvalerophenone is described. The process described is a three step process comprising the synthesis of organomagnesium specie, coupling reaction between the organomagnesium specie and trifluoromethylbenzonitrile or trifluoromethylbenzoyl chloride and preferably a purification of the product obtained in suitable reaction conditions. In the process an extraction phase of the final product is not required.
专利号:US-4822903-A 优先权日:1981-05-15 标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof 发明人:JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT 权利人:RHONE POULENC SPEC CHIM 摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.
专利号:US-6380436-B1 优先权日:1998-05-12 标 题 :Process for the synthesis of alkoxyalkyl (trifluormethylphenyl) methanones 发明人:THENNATI RAJAMANNAR; DEO KESHAV; MIDHA AJAY SOHANLAL; CHANDRA TILAK; PATEL VIJAY MULJIHHAI 权利人:SUN PHARMACEUTICAL IND LTD 摘要:A new process is described for the preparation of (alkoxyalkyl)(4-trifluoromethylphenyl)methanones. The process comprises reacting a 4-trifluoromethylbenzonitrile with an alkoxyalkyl Grignard in the presence of a suitable polar aprotic solvent. The compound (4-methoxybutyl)(4-trifluoromethylphenyl)methanone is useful as an intermediate in the preparation of the antidepressant drug fluvoxamine.
专利号:US-7074931-B2 优先权日:2000-08-02 标 题:Process for asymmetric synthesis of substituted 1,4 -dihydropyridines 发明人:PATEL IAN; ASHWORTH IAN; LEVIN DANIEL 权利人:ASTRAZENECA AB 摘要:A process is described for reacting a vinylogous amide with an α,β-unsaturated ketone in the presence of a silicon compound to form an 1,5-diketone which is converted to a 1,4-dihydropyridine. Asymmetric substituted 1,4-dihydropyridines are synthesized by the process by preparing an asymmetric vinylogous amide by reacting a 1,3-cyclohexanedione with a substantially homo-chiral phenylethylamine. Reaction of the asymmetric vinylogous amide with an α,β-unsaturated ketone in the presence of a silicon compound forms an asymmetric 1,5-diketone. The 1,5-diketone is converted to an asymmetric substituted 1,4-dihydropyridine.
专利号:US-2004039207-A1 优先权日:2000-08-02 标 题:Process for asymmetric synthesis of substituted 1,4 -dihydropyridines
[参考文献]: Nobuyuki Ishikura, Et Al. Ch5137291, An Androgen Receptor Nuclear Translocation-Inhibiting Compound, Inhibits The Growth Of Castration-Resistant Prostate Cancer Cells. Int J Oncol. 2015 Apr;46(4):1560-72.
合成参考文献
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