戊腈置于copper Chromite,乙醚,氨,镍体系中,125.0~180.0 °C,12.26 Mpa 条件下,反应生成N-乙基戊胺 参考文献:Preparation Of Certain Amines 标题:Preparation Of Certain Amines 摘要: Doi:10.1021/ja01267A081
专利号:US-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
专利号:US-4231955-A 优先权日:1979-07-13 标题 :Synthesis of alkyl and alkylaminonitriles 发明人:CHANG CLARENCE D; LANG WILLIAM H; LAPIERRE RENE B 权利人:MOBIL OIL CORP 摘要:A method is provided for synthesizing alkylnitriles and alkylaminonitriles by reacting formaldehyde, a C1-C5 monohydric alcohol and a compound having the formula R1R2NH where R1 and R2 are selected from the group consisting of hydrogen and alkyl groups containing 1 to 5 carbon atoms under effective conditions in the presence of a catalyst comprising a crystalline aluminosilicate zeolite having a silica to alumina ratio of at least about 12 and a constraint index within the approximate range of 1 to 12 and recovering from the resulting reaction mixture, a product containing at least one of the above nitrile compounds.
专利号:US-5808071-A 优先权日:1996-09-27 标题 :Pictet-Spengler reaction for the synthesis of tetrahydroisoquinolines and related heterocyclic compounds 发明人:WATSON TIMOTHY JAMES-NORMAN 权利人:HOECHST MARION ROUSSELL INC 摘要:A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of a suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.
专利号:EP-0929527-B1 优先权日:1996-09-27 标题 :Pictet-spengler reaction for the synthesis of tetrahydroisoquinolines and related heterocyclic compounds 发明人:WATSON TIMOTHY JAMES-NORMAN 权利人:AVENTIS PHARMA INC 摘要:A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.
专利号:US-5530125-A 优先权日:1992-02-25 标 题 :Synthesis of α-substituted-aryl ethylamines 发明人:BERGER JOEL G; CHANG WEI K; KOZLOWSKI JOSEPH A; ZHOU GUOWEI 权利人:SCHERING CORPORTION 摘要:PCT No. PCT/US93/01425 Sec. 371 Date Aug. 19, 1994 Sec. 102(e) Date Aug. 19, 1994 PCT Filed Feb. 23, 1993 PCT Pub. No. WO93/16997 PCT Pub. Date Sep. 2, 1993.A novel process for the preparation of alpha -substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the alpha -carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R4-X, wherein R4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The alpha -substituted arylacetamides are useful as intermediates in the preparation (by reduction) of alpha -substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R4 is 1-(1-cycloalkenyl) are novel.
专利号:US-5973166-A 优先权日:1998-03-02 标 题 :Method for the preparation of maleimides 发明人:MIZORI FARHAD G; DERSHEM STEPHEN M 权利人:DEXTER CORP 摘要:In accordance with the present invention, there are provided improved methods for the preparation of maleimide monomers. This new method for the synthesis of maleimides is clearly superior to those documented in the prior art. Furthermore, the invention method utilizes materials with reduced toxicity, thus the overall process has a minimal impact on the environment. Thus, in accordance with the present invention, it has been discovered that certain amine salts can be successfully used to replace the polar, aprotic solvents cited in the prior art for the cyclodehydration of maleamic acids. The use of these salts provides competitive reaction times and product yields relative to results obtained with the polar, aprotic solvents. These salts have the advantage of having no vapor pressure and, therefore, have no possibility to co-distill with the water produced by the cyclodehydration reaction. Furthermore, such salts can be tailored to have desirable solubility characteristics (i.e., soluble in the refluxing azeotropic solvent, but insoluble at room temperature) that permit their easy removal from the reaction product. Such salts are not destroyed during the cyclodehydration reaction and, therefore, can be efficiently recycled again and again.