2,4-二氧代-3-氮杂螺[5.5]十一烷-1,5-二甲腈置于盐酸,水,乙酸酐,溶剂黄146体系中,化学反应 88.0H,反应生成1,1-环己基二乙酸酐 参考文献:Antiarthritic And Supressor Cell Inducing Activity Of Azaspiranes: Structure-Function Relationships Of A Novel Class Of Immunomodulatory Agents 标题:Antiarthritic And Supressor Cell Inducing Activity Of Azaspiranes: Structure-Function Relationships Of A Novel Class Of Immunomodulatory Agents 摘要:Spirogermanium (1; 8,8-Diethyl-N,N-Dimethyl-2-Aza-8-Germaspiro[4.5]Decane-2-Propanamine Dihydrochloride) Is A Potent Cytotoxic Agent In Vitro Which Has Demonstrated Limited Activity In Experimental Animal Tumor Models. Subsequently,It Has Been Reported That Spirogermanium Has Antiarthritic And Suppressor Cell-Inducing Activity. We Have Synthesized A Series Of Substituted 8-Hetero-2-Azaspiro[4.5]Decane And 9-Hetero-3-Azaspiro[5.5]Undecane Analogues Of Spirogermanium To Identify The Heteroatom Requirements For In Vivo Antiarthritic And Suppressor Cell-Inducing Activity. This Structure-Activity Relationship Study Has Identified That Appropriately Substituted Silicon And Carbon Analogues Of Spirogermanium Retain Both Antiarthritic And Immunosuppressive Activity,With The 8,8-Dipropyl (Carbon) Analogue Being Among The Most Active. Following The Identification Of N,N-Dimethyl-8,8-Dipropyl-2-Azaspiro[4.5]Decane-2-Propanamine++ + Dihydrochloride (9) As A More Active Analogue Than Spirogermanium,A Series Of 8,8-Dipropyl Analogues With Various Amine Substituents Were Synthesized. A Number Of These Analogues Had Activity Similar To That Of 9. A Correlation Between Activity In The Adjuvant Arthritic Rat And The Ability To Induce Suppressor Cells (R = 0.894,P Less Than 0.001) Suggests An Association Between The Two Pharmacologic Effects. While The Precise Biochemical Mechanism(S) For The Pharmacological Activity Is Unclear,These Data Suggest That Compounds Within This Series,E.G.,N,N-Dimethyl-8,8-Dipropyl-2-Azaspiro[4.5]Decane-2-Propanamine++ + Dihydrochloride,May Provide Effective Therapy In Diseases Of Autoimmune Origin And/or The Prevention Of Rejection In Tissue Transplantation. Doi:10.1021/jm00173A010
专利号:US-2008103334-A1 优先权日:2006-10-26 标 题:Process For Synthesis Of Gabapentin 发明人:KUMAR ASHOK; SOUDAGAR SATISH RAJANIKANT; NIJASURE AVINASH MANOHAR; PANDA NALINAKSHYA BALARAM; GAUTAM PRASHANT; THAKUR GAJENDRASINGH RAMSINGH 权利人:IPCA LAB LTD 摘要:A process for preparation of gabapentin comprising a step of obtaining 1,1-cyclohexane diacetic acid monoamide from 1,1-cyclohexane diacetic acid anhydride, wherein said reaction is characterized by the use of ammonia precursor or pre-generated ammonia-isopropanol solution. The invention further discloses preparation of gabapentin and isolation of gabapentin in polymorphic Form II with high yield and purity.
专利号:US-7759517-B2 优先权日:2004-06-24 标 题:Process for the preparation of gabapentin 发明人:VILLA MARCO; PAIOCCHI MAURIZIO; ARRIGHI KATIUSCIA; CORCELLA FRANCESCO; CANNATA VINCENZO; SORIATO GIORGIO; VERZINI MASSIMO 权利人:ZACH SYSTEM SPA 摘要:The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of α, -diaminocarbonyl-β,β-pentamethylene glutarimide.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:US-2005239725-A1 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
专利号:US-4810778-A 优先权日:1986-01-16 标 题 :Intermediates for preparing 1,6-dicarba-vasopressin compounds 发明人:CALLAHAN JAMES F; HUFFMAN WILLIAM F; NEWLANDER KENNETH A; YIM NELSON C F 权利人:SMITHKLINE BECKMAN CORP 摘要:New compounds which have potent V2-vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by the Pas1,6 or Tas1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
专利号:US-4760052-A 优先权日:1986-01-16 标 题 :1,6-dicarba-vasopressin compounds 发明人:CALLAHAN JAMES F; HUFFMAN WILLIAM F; NEWLANDER KENNETH A; YIM NELSON C F 权利人:SMITHKLINE BECKMAN CORP 摘要:New compounds which have potent V2-vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by a Pas1,6 or Tas1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.