三甲基苯甲氧基胺置于盐酸体系中,用 甲醇 作为反应溶剂,化学反应 0.5H,以73%的收率获得产物苄基三甲基氯化铵 参考文献:Competing Pathways In The Azomethine Ylide Route To Indoloquinones: An Improved Procedure For The Generation Of A Transient 4-Oxazoline From The Oxazolium Salt 标题:Competing Pathways In The Azomethine Ylide Route To Indoloquinones: An Improved Procedure For The Generation Of A Transient 4-Oxazoline From The Oxazolium Salt 摘要:Azomethine Ylide Generation From The Oxazolium Salt 22 And Phsih3/csf Affords Complex Products Derived From The Initial Cycloadduct 23 Via Three Competing Pathways. Colorless Intermediates 24-27 Have Been Detected,And Their Oxidation Products 10,28,And 29 Have Been Identified. Nucleophilic Activation Of The Oxazolium Salt 22 Is Reported Using The Organic-Soluble Benzyltrimethylammonium Cyanide. This Variation Affords The Unstable Cycloadduct 32,Which Undergoes Aromatization Via A Single Pathway Involving 24 And 27,And Ddq Oxidation Gives The Indoloquinone 10 In An Improved 63% Yield. Lower Yields Using Phsih3/csf Or Nacn Activation Methods Are Attributed To The Heterogeneous Conditions And Interception Of The Azomethine Ylide By Unreacted Oxazolium Salt. DOI:10.1021/jo9702195
专利号:US-2008103312-A1 优先权日:2006-08-29 标 题:Processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole 发明人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 权利人:KANSAL VINOD K; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; LUNAGARIYA VIJAYKUMAR D 摘要:Provided are processes for the synthesis of 5-phenyl-1-trityl-1H-tetrazole, an intermediate useful in the synthesis of irbesartan.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-4284582-A 优先权日:1978-04-28 标 题 :Process for the preparation of cyclopropane derivatives, intermediates in the synthesis of pyrethroid insecticides 发明人:KAYE ALBERT E; TUCKER ALAN C 权利人:ICI LTD 摘要:Compounds of formula: wherein both groups X are chlorine, bromine or trifluoromethyl, or one X is chlorine or bromine and the other is trifluoromethyl, and Y is -CN or -COOR in which R is an alkyl group, are obtained by (A) reacting a compound of the formula: wherein X1 is chlorine or bromine, with a compound of the formula: X2C=CH-CH=C(CH3)2 in the presence of metallic copper or at least one copper salt and a base, or (B) reacting a compound of the formula: Y-CH2-CN with a compound of the formula: X2C=CH-CH=C(CH3)2 and chlorine or bromine, in the presence of at least one reducible copper salt and a base, or (C) reacting a compound of formula: X-CH2-CN with a compound of the formula: wherein X1 is chlorine or bromine, in the presence of at least one copper salt. The compounds are intermediates in the synthesis of pyrethroid insecticides.
专利号:US-4422970-A 优先权日:1982-05-20 标题 :Method of synthesis of 1-dodecylazacycloheptan-2-one 发明人:RAJADHYAKSHA VITHAL J; PECK JAMES V; MINASKANIAN GEVORK 权利人:NELSON RES & DEV 摘要:In a method of synthesis of 1-substituted azacycloalkan-2-ones with primary alkyl halides and aralkyl halides as alkylating agents, the improvement comprising carrying out the N-alkylation in the presence of a phase transfer catalyst having the structural formula where X is suitable anion; and R1, R2, R3 and R4 are each alkyl or aralkyl groups having 1-18 carbon atoms, or R2, R3 and R4 can form a part of a heterocyclic ring, with the proviso that the combined total of carbon atoms is between 16 and 40.
专利号:US-4939112-A 优先权日:1988-10-06 标 题:Catalyst for synthesis of vesicular phenoxy resins 发明人:BENNETT EVERETT W 权利人:JAMES RIVER PAPER CO 摘要:A catalyst for synthesis of vesicular phenoxy resins is disclosed. The catalyst includes a water-insoluble complex of a hydric phenol and a quaternary ammonium or phosphonium salt of the hydric phenol. Preferably, the hydric phenol is an intermediate of the phenoxy resin being produced. Dihydric phenols, such as sulfonyldiphenol are preferred. The invention further relates to a reaction medium for polymerization of phenoxy resins including the above-described catalyst and a solvent medium capable of dissolving the phenoxy resins and otherwise not interfering with the polymerization reaction. The solvent medium is advantageously free of toxic Methyl Cellosolve.