CAS: 4355-11-7; 1,1-Cyclohexanediaceticacid

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2,4-二氧代-3-氮杂螺[5.5]十一烷-1,5-二甲腈置于盐酸,水,溶剂黄146体系中,化学反应 84.0H,反应生成 1,1-环己基二乙酸
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

专利信息

专利号:US-6846950-B2
优先权日:2002-10-01
标题 :Process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride
发明人：FERRARI MASSIMO; GHEZZI MARCELLO; BELOTTI PAOLO
权利人:ERREGIERRE SPA
摘要:A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising:n a) Reaction of a mixture of acetic anhydride/ammonium acetate with 1,1-cyclohexane-diacetic acid to yield 3,3-pentamethylene glutarimide; b) Treatment of 3,3-pentamethylene glutarimide with sodium hydroxide in an aqueous solution up to dissolution, dripping the solution thus obtained into a sodium hydroxide/sodium hypochlorite mixture, which is also aqueous, followed by acidification with hydrochloric acid to yield gabapentine hydrochloride.

专利号:US-2005009154-A1
优先权日:2003-06-19
标 题:Biocatalytic preparation of 1-cyano-cyclohexaneacetic acid
发明人：WONG JOHN WING; BURNS MICHAEL PAUL
权利人:PFIZER
摘要:The present invention is directed to novel biocatalytic processes for the conversion of aliphatic âˆ?, ω-dinitriles into the corresponding ω-nitrilecarboxylic acid. More particularly, the present invention provides a method for the conversion of 1-cyanocyclohexaneacetonitrile to 1-cyanocyclohexaneacetic acid using an enzyme catalyst with nitrilase activity. 1-cyanocyclohexaneacetic acid is a useful intermediate in the synthesis of gabapentin.

专利号:US-6177572-B1
优先权日:1997-08-20
标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use
发明人：WANG FENGJIANG
权利人:SEPRACOR INC
摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.

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.