专利号:US-4125735-A 优先权日:1975-03-20 标 题 :Synthesis of esters of acetylenic alcohols 发明人:CLOSE RALPH E; OROSHNIK WILLIAM 权利人:SCM CORP 摘要:A process for the synthesis of perfume products, Vitamin E and intermediates described herein involving a coupling reaction. For instance, a process for the synthesis of dehydrophytol and Vitamin E comprising forming a C15 acetylene from hexahydropseudoionone and then coupling said acetylene with 1-acetoxy-4-chloro-3-methylbut-2-ene to form a C20 acetoxy-enyne. The latter is readily subjected to partial hydrogenation and saponification in that order to form a dehydrophytol, a useful intermediate for the synthesis of Vitamin E and other products.
专利号:US-4039591-A 优先权日:1975-03-20 标 题:Synthesis of dehydrophytol and Vitamin E 发明人:CLOSE RALPH E; OROSHNIK WILLIAM 权利人:SCM CORP 摘要:A process for the synthesis of dehydrophytol and Vitamin E comprising forming a C15 acetylene from hexahydropseudoionone and then coupling said acetylene with 1-acetoxy-4-chloro-3-methylbut-2-ene to form a C20 acetoxy-enyne. The latter is readily subjected to partial hydrogenation and saponification in that order to form a dehydrophytol, a useful intermediate for the synthesis of Vitamin E and other products.
专利号:US-4115466-A 优先权日:1975-10-16 标题:Synthesis of acetylenic compounds useful in preparing dehydrophytols and Vitamin E 发明人:CLOSE RALPH E; OROSHNIK WILLIAM 权利人:SCM CORP 摘要:A process for the synthesis of an acetylenic hydrocarbon from an acetylenic carbinol which involves first replacing the hydroxyl group of the carbinol with a halogen to form a propargylic halide, dehalogenating the propargylic halide to form an allene, and isomerizing said allene to the desired acetylene. The present invention is particularly useful in the synthesis of Vitamin E.
专利号:US-4056573-A 优先权日:1975-04-24 标题:Synthesis of acyclic, terpene alcohols 发明人:CLOSE RALPH E; DERFER JOHN M 权利人:SCM CORP 摘要:Shown is a process for the synthesis of acyclic, terpene alcohols, such as 3,7-dimethyloctan-1-o1 and 7-substituted hydroxy or ethoxy derivatives thereof, wherein 3-methylbut-1-yn or the 3-substituted hydroxy or ether derivative thereof is coupled with a C5 coupling reagent having the configuration X being a leaving group such as chloride, bromide, iodide, tosylate and mesylate; R being or OR', R' being a lower alkyl up to 5 carbon atoms, phenyl, substituted phenyl up to 10 carbon atoms, cycloalkyl or aralkyl up to 10 carbon atoms, followed by hydrogenation and saponification or deetherification.
专利号:US-2010010212-A1 优先权日:2005-09-08 标题 :Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe 发明人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN 权利人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN 摘要:The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompasses processes for preparing Compound 2a from Compound 1 having the following formula: n n n n n n n n n n The invention also encompasses processes for preparing a compound having the following formula: n n n n n n n n n n from a compound having the following formula: n n n n n n n n n n wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions
专利号:US-8293739-B2 优先权日:2006-12-28 标题:Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof 发明人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON 权利人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON; KINEX PHARMACEUTICALS LLC 摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy) phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.
摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 803. 摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#02788