Spiro[cyclohexane-1,9'-(3,7-Diazabicycle-[3.3.1]Nonane)]-2',4',6',8'-Tetraone置于水,Sodium Hydroxide体系中,化学反应 18.0H,以80.8%的收率获得产物1,1-环己基二乙酸单酰胺 参考文献:Process For The Preparation Of Gabapentin 标题:Process For The Preparation Of Gabapentin 摘要:本发明涉及一种改进的加巴喷丁制备工艺.该工艺还涉及一种新的1,1-环己烷二乙酸单酰胺(cdma)制备工艺,该工艺是制备加巴喷丁的关键中间体.
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-7381823-B2 优先权日:2004-03-17 标 题 :Process for preparing cyclohexanediacetic acid monoamide 发明人:DANIELI BRUNO; DELOGU PIETRO; ROSA SABRINA DE; FUGAZZA LORENZA 权利人:SERICHIM S R L 摘要:A new process is described for synthesising cyclohexanediacetic acid monoamide, a key compound in the synthesis of grabapentin precursors. The process of the invention is characterised by reacting cyclohexanone with cynoacetamide and immediately after, with a suitable malonic acid ester. A new intermediate (5-cyano-2,4-dioxo-3-azaspiro[5,5]undecane-1-carboxylic acid ester) is obtained which is convertible, under mild reaction conditions, into cyclohexanediacetic acid monoamide.