专利号:WO-9910310-A1 优先权日:1997-08-29 标 题:Process for producing diphenylethers and esters 发明人:LOURENS GERHARDUS JOHANNES 权利人:DOW CHEMICAL CO 摘要:An improved synthesis of diphenylethers, and in particular, the bacteriostat 2,4,4'-trichloro-2'-hydroxydiphenylether, is described wherein 2'-acetyl-2,4,4'-trichlorodiphenylether is oxidised under Baeyer-Villiger conditions to produce 2'-acetoxy-2,4,4'-trichlorodiphenylether in near quantitative yield. Best oxidative conditions include the use of anhydrous permaleic acid produced in situ. The ester is purified readily by simple recrystallization, as no dibenzofurans and only minor amounts of byproducts are formed in the process. The ester is converted into the desired halogenated phenolic diphenylether, 2,4,4'-trichloro-2'-hydroxydiphenylether, by hydrolysis or transesterification. The final product is purified to a high degree by vacuum distillation and crystallization to meet current purity standards for approved applications.
专利号:US-2025188083-A1 优先权日:2021-06-25 标 题:Modulators of Histone Acetyltransferase 1 and Methods of Treatment Thereof 发明人:GRUBER JOSHUA JAMES; LIPCHIK ANDREW; SNYDER MICHAEL P; SCHOW STEVEN R 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Small molecules compounds and methods of their synthesis are provided. Small molecules identified can inhibit histone acetyltransferase 1 activity. Formulations and medicaments are also provided that are directed to the treatment of human disorders and conditions, such as, for example, neoplasms, cancers, viral, fungal, and parasitic infections, and aging. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
专利号:RU-2193549-C2 优先权日:1997-02-05 标 题 :Method of synthesis of halide-substituted compounds of hydroxybiphenyl
专利号:US-10072009-B2 优先权日:2014-10-21 标 题 :N-substituted beta-carbolinium compounds as potent P-glycoprotein inducers 发明人:BHARATE SANDIP; KUMAR AJAY; MANDA SUDHAKAR; JOSHI PRASHANT; BHARATE SONALI; VISHWAKARMA RAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to the N-substituted beta-carbolinium compounds of general formula A and formulae I and II wherein, R 1 and R 2 groups are selected from halogens or trifluoromethyl; R 3 group is selected from hydrogen or methyl; Ar is selected from aryl and heteroaryl, X is selected from halogens; and R 1 and R 2 groups may be attached to any position on ring E. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the N-substituted beta-carbolinium compounds. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.
专利号:US-5734067-A 优先权日:1994-09-28 标题 :Anti-oxidative tricyclic, condensed heterocyclic compound 发明人:JINNO SHUJI; KOGURE YASUYO; ONUKI HIROYUKI; OKITA TAKAAKI 权利人:NIPPON SUISAN KAISHA LTD 摘要:Providing a novel tricyclic, condensed heterocyclic compound having an anti-oxidative action and being promising for use in pharmaceutical agents, cosmetics, chemical products and the like. By chemical synthesis, a novel anti-oxidative, tricyclic, condensed heterocyclic compound represented by the following formula: ##STR1## (wherein X--Y represents CH 2 --Câ•?O, CH 2 --CH 2 or CHâ•?CH; Z represents O, S, or Sâ•?O; R 1 to R 8 represent independently those selected from the group consisting of hydrogen atom, a hydroxyl group, a halogen group, a lower alkyl group, a lower alkoxyl group, a lower alkyl ketone group and CF 3 ; and at least two of R 1 to R 4 are hydroxyl groups); and the salts thereof are provided. The compound has an anti-oxidative activity at the same degree as or higher than the activity of α-tocopherol, so the compound is promising as a therapeutic drug for a variety of diseases, such as cancer, arteriosclerosis, or liver diseases, in which it is believed that biological lipid peroxides may b involved.
专利号:US-7825149-B2 优先权日:2006-01-19 标 题 :Substituted imidazoles 发明人:CHUBB NATHAN ANTHONY LOGAN; COX MARK ROGER; DAUVERGNE JEROME SEBASTIEN; EWIN RICHARD ANDREW; LAURET CHRISTELLE 权利人:PFIZER LTD 摘要:This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
参考标题:Metal-Free Activation Of C(Sp3 )-H Bond, And A Practical And Rapid Synthesis Of Privileged 1-Substituted 1,2,3,4-Tetrahydroisoquinolines 作者:Santosh Kumar Choudhury,Pragati Rout,Bibhuti Bhusan Parida,Jean-Claude Florent,Ludger Johannes,Ganngam Phaomei,Emmanuel Bertounesque,Laxmidhar Rout |发布日期:2017.9.25 摘要:Reaction Of Cotarnine And Acyl/aryl Ketones In Green Solvents Provides An Efficient Approach To An Array Of Privileged 1,2,3,4-Tetrahydroisoquinolines In Excellent Yields By Metal Free Activaion Of C(Sp3)-H Bonds. This One-Pot Procedure Takes Place Under Base-Free Conditions At Room Temperature, And Tolerates A Wide Range Of Functionalities. The Reaction Is Highly Chemo-Selective, Scalable In Multi-Gram
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 360.