4,4'-二羟基联苯 反应生成4-(4-羟基苯基)环己酮 参考文献:Process For Producing Alicyclic Monoketones And Process For Producing Alicyclic Diketones 标题:Process For Producing Alicyclic Monoketones And Process For Producing Alicyclic Diketones 摘要:根据本发明,制备脂环单酮(羟基苯基环己酮衍生物)的方法包括在溶剂中,在帕拉铂/碱金属催化剂的存在下,加氢取代双酚,如双酚a,其中帕拉铂和碱金属都负载在载体上,以获得脂环单酮,如2-(4-氧代环己基)-2-(4-羟基苯基)丙烷.根据本发明,制备脂环二酮的方法包括在溶剂中,在帕拉铂/碱金属催化剂的存在下,加氢取代双酚,如双酚a,其中帕拉铂和碱金属都负载在载体上,以获得脂环二酮,如2,2-双(4-氧代环己基)丙烷和4,4'-双环己酮.根据本发明,制备脂环单酮的另一方法包括在有机溶剂中,在帕拉铂催化剂的存在下,加氢双苯酚,如双(4-羟基苯基),其中10至30%的重量的帕拉铂负载在载体上,以获得脂环单酮,如4(4'-羟基苯基)环己酮.根据本发明,通过简单的步骤可以以高选择性和高产率获得脂环单酮或脂环二酮,因为该过程只包括一个反应步骤,在相对温和的条件下加氢取代双酚.
专利号:WO-2013014486-A1 优先权日:2011-07-28 标题:Improved synthesis of 2-(4-(4-chlorophenyl) cyclohex-1-enyl) -3, 4-dihydronaphthalen-1 (2h)-one; an intermediate for atovaquone 发明人:ROY BHAIRAB NATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; TRIVEDI AUNRAG 权利人:LUPIN LTD; ROY BHAIRAB NATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; TRIVEDI AUNRAG 摘要:A process for preparation of 2-(4-(4-chlorophenyl) cyclohex-l-enyl)-3,4-dihydronaphthalen- 1(2H)-one (V), key intermediate for synthesis of Atovaquone [I]. The process for preparation of compound(V) comprising of the steps of; i) Reaction of 2-(4-(4-chlorophenyl)-1-hydroxycyclohexyl)-3,4-dihydronaphthalen- 1(2H)-one (IV) with trifluro acetic anhydride in presence of base in organic solvent to yield compound of formula (XIa) ii) Elimination of trifluoroacetyl functionality of compound (XIa) in organic solvent and in presence of organic base to give compound of formula (V). The invention also provides a Process for preparation of compound(XIa) comprising of the steps of; i) reaction of 2-(4-(4-chlorophenyl)-l-hydroxy cyclohexyl)-3,4-dihydronaphthalen- 1(2H)-one (IV) with trifluro acetic anhydride in presence of organic base in organic solvent. A further process is provided for preparation of compound(V) from compound (XIa) comprising elimination reaction of trifluoroacetyl functionality compound (XIa) in organic solvent and in presence of organic base.
专利号:US-9321728-B2 优先权日:2012-04-25 标题:Beta-alanine derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical composition comprising same as active ingredient 发明人:AHN JIN HEE; PAGIRE H S; RHEE SANG DAL; KIM KI YOUNG; JUNG WON HOON; BAE MYUNG-AE; SONG JIN SOOK; KIM KWANG-ROK; KWAK HYUN JUNG 权利人:KOREA RES INST CHEM TECH; HANDOK PHARMACEUTICALS CO LTD 摘要:The present invention relates to a beta-alanine derivative, pharmaceutically acceptable salts thereof, and a pharmaceutical composition including the same as an active ingredient. The novel beta-alanine derivative and pharmaceutically acceptable salts thereof according to the present invention may effectively inhibit the activity of DGAT1, which is an enzyme serving as a catalyst in the final step of the synthesis of neutral lipids, to thereby be effectively used as a pharmaceutical composition for preventing or treating various lipid metabolism-related disorders selected from the group consisting of obesity, dyslipidemia, fatty liver, insulin resistance syndrome, and hepatitis.
专利号:CN-106892805-B 优先权日:2015-12-19 标题 :Synthesis method of 4- (4-hydroxyphenyl) cyclohexanone
专利号:CN-111777498-A 优先权日:2019-04-04 标题:Synthesis and purification method of 4- (4-hydroxyphenyl) cyclohexanone
参考文献:10.1021/acs.jmedchem.7b01601 摘要:Hanson AM, Perera KLIS, Kim J, Pandey RK, Sweeney N, Lu X, Imhoff A, Mackinnon AC, Wargolet AJ, Van Hart RM, Frick KM, Donaldson WA, Sem DS. A–C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions. J. Med. Chem. 2018 May 09;61(11):4720–38. doi: 10.1021/acs.jmedchem.7b01601.