3-溴苯硼酸置于三氟化硼乙醚,Sodium Hydride体系中,用 二氯甲烷,甲基叔丁基醚,Mineral Oil 用作溶剂,化学反应 1.75H,反应生成间溴苯甲醚 参考文献:Base Mediated Synthesis Of Alkyl-Aryl Ethers From The Reaction Of Aliphatic Alcohols And Unsymmetric Diaryliodonium Salts 标题:Base Mediated Synthesis Of Alkyl-Aryl Ethers From The Reaction Of Aliphatic Alcohols And Unsymmetric Diaryliodonium Salts 摘要:The Base Mediated Coupling Of Aliphatic Alcohol Pronudeophiles With Unsymmetric Diaryliodonium Salt Electrophiles Is Described. This Metal-Free Reaction Is Operationally Simple,Proceeds At Mild Temperature,And Displays Broad Substrate Scope To Generate Industrially Important Alkyl-Aryl Ethers In Moderate To Excellent Yield. The Synthetic Utility Of These Reactions Is Demonstrated,And Aspects Of Sustainability Are Highlighted By The Use Of Unsymmetric Aryl(Mesityl)Iodonium Arylating Reagents. Doi:10.1021/acs.Joc.5B00907
专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:US-8791287-B2 优先权日:2010-07-02 标 题:Process for the synthesis of tapentadol and intermediates thereof 发明人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; LANDONI NICOLA 权利人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; LANDONI NICOLA; EUTICALS SPA 摘要:The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. n A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention. n Still another object of the invention is represented by the crystalline forms I and II of the tapentadol free base. n A further object of the present invention is the mixture of the crystalline forms I and II of the tapentadol free base.
专利号:US-2013296608-A1 优先权日:2011-01-27 标 题 :Novel stereospecific synthesis of (-) (2s, 3s)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol 发明人:MOHAN RAO DODDA; KRISHNAREDDY PINGILI; RAMACHANDRAREDDY PINGILI; HARITHA KIRLA; SRINIVAS KOLLURU 权利人:MOHAN RAO DODDA; KRISHNAREDDY PINGILI; RAMACHANDRAREDDY PINGILI; HARITHA KIRLA; SRINIVAS KOLLURU; SYMED LABS LTD 摘要:The present invention relates to a novel stereospecific synthesis of (−)(2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol an intermediate in the synthesis of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol.
专利号:US-6417380-B1 优先权日:1987-12-31 标 题 :Synthesis of 1,2-dioxetanes and intermediates therefor 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 摘要:Compounds having the formula: n wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., n m-phenylene), produced by reacting a compound having the formula: n with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: n are produced by reacting a compound having the formula: n with n wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula n are produced by reacting a compound of the formula n with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
专利号:WO-2024140771-A1 优先权日:2022-12-30 标 题 :Catalyst for synthesis of polyimide, preparation method therefor and use thereof 发明人:DUAN PINGPING; HE JUNPENG; DING MINGYUE; WU HONGSHENG 权利人:BYD CO LTD 摘要:A catalyst for synthesis of polyimide. The structural formula of the catalyst is as shown in formula (I), wherein Ar 1 and Ar 2 are independently selected from a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic aryl group, and R 1 is oxygen, sulfur, a sulfone group, a sulfoxide group, a carbonyl group, a secondary amine group, an alkylene group, an alkenylene group, an alkynylene group, an alicyclic group, a heterocycloarylene group, a fused ring arylene group, or a single bond.
专利号:US-5777133-A 优先权日:1987-12-31 标 题:Synthesis of 1, 2-dioxetanes and intermediates therefor 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 权利人:TROPIX INC 摘要:Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (eg., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
摘要:Li, Y.; Xie, W.; Jiang, X., Science of Synthesis Knowledge Updates, (2016) 2, 8. 摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 68. 摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 50. 摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 99. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 35.