3,5-二甲氧基苯胺置于亚硝酸,Copper(I) Bromide体系中,用33%的收率获得1-溴-3,5-二甲氧基苯 参考文献:The Photochemistry Of 1-(3,5-Dimethoxyphenyl)-2-(4-Methoxyphenyl)Ethyl Ethanoate In Alcohol Solvents: A Search For Carbocation Rearrangements 标题:The Photochemistry Of 1-(3,5-Dimethoxyphenyl)-2-(4-Methoxyphenyl)Ethyl Ethanoate In Alcohol Solvents: A Search For Carbocation Rearrangements 摘要:标题化合物1在甲醇和2,2,2-三氟乙醇中的光化学性质已经被研究.在两种溶剂中,都得到了两种醚产物:一种(18)是由于捕获了碳阳离子2(从1的光溶解预期而来),另一种(19)是由于碳阳离子3(在阳离子2的氢迁移重排后预期而来)而产生的.取代的反-和顺-苯乙烯衍生物20和21也是主要的光产物.随着时间的推移,对产物产率的分析表明,醚产物19是通过反式-苯乙烯衍生物的二次光解产生的,可能是通过涉及激发态质子化的途径.纳秒激光脉冲光解实验结果表明,取代的反式-苯乙烯20在与激光脉冲相同的时间尺度上产生.关键词:酯光化学,苯乙烯光加成,碳阳离子重排. Doi:10.1139/v03-072
专利号:US-8530689-B2 优先权日:2008-05-05 标 题 :Processes for the preparation of biphenyl compounds 发明人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J 权利人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J; UNIV PENNSYLVANIA 摘要:The invention concerns processes for the synthesis of a compound of the formula: wherein: R 1 and R 2 are each, independently, C 1 -C 12 alkyl, CO 2 R 3 , OR 4 , R 5 (OR 6 ), or C 6 -C 18 aryl; R 3 -R 6 are each, independently, C 1 -C 12 alkyl or C 6 -C 12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R 7 -0H with BH 3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R 7 is a C 2 -C 12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.
专利号:US-7884125-B2 优先权日:2008-04-30 标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues 发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS 权利人:UNIV GENT 摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:WO-2020031179-A1 优先权日:2018-08-06 标题:Methods for synthesis of cannabinoid compounds 发明人:JAGTAP PRAKASH; MUSA SANAA 权利人:BEETLEBUNG PHARMA LTD 摘要:The present invention provides simple synthetic routes for the preparation of cannabinoid compounds such as CBD, CBDV, THC, THCV, CBN, HU-308, CBG, CBC, and derivatives thereof, which are stereoselective and provide the desired cannabinoid compound in high yield.
专利号:US-9428500-B2 优先权日:2012-05-11 标 题 :Alpha-carbolines for the treatment of cancer 发明人:GAMBACORTI-PASSERINI CARLO; MOLOGNI LUCA; SCAPOZZA LEONARDO; BISSON WILLIAM; AHMED SHAHEEN; GOEKJIAN PETER; TARDY SÉBASTIEN; ORSATO ALEXANDRE; GUEYRARD DAVID; BENOIT JOSEPH 权利人:UNIVERSITA' DEGLI STUDI DI MILANO—BICOCCA; UNIV GENEVE; UNIVERSITÉ CLAUDE BERNARD—LYON 1; UNIV DEGLI STUDI DI MILANO—BICOCCA; UNIV GENEVE; UNIV CLAUDE BERNARD—LYON 摘要:The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.
专利号:US-9062085-B2 优先权日:2010-09-10 标 题 :Biaryl diphosphine ligands, intermediates of the same and their use in asymmetric catalysis 发明人:ABDUR-RASHID KAMALUDDIN; JIA WENLI; LU SHUIMING; GUO RONGWEI; CHEN XUANHUA; AMOROSO DINO 权利人:ABDUR-RASHID KAMALUDDIN; JIA WENLI; LU SHUIMING; GUO RONGWEI; CHEN XUANHUA; AMOROSO DINO; KANATA CHEMICAL TECHNOLOGIES INC 摘要:The present disclosure relates to biaryl diphosphine ligands of the formula (B), processes for the production of the ligands and the use of the ligands in metal catalysts for asymmetric synthesis. The disclosure also relates to intermediates used for the production of the biaryl diphosphine ligand. (Formula (B))
专利号:US-2009275616-A1 优先权日:2008-04-30 标 题 :Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues