CAS: 60142-95-2; 2-[1-(Aminomethyl)Cyclohexyl]Acetic Acid,Hydrochloride

📜3,3'-亚戊烯基-4-丁内酰胺置于盐酸,水体系中,化学反应 24.0H,以90%的收率获得产物加巴喷丁盐酸盐
参考文献:催化碱金属溴化物对酰亚胺的霍夫曼型重排的影响.
标题:催化碱金属溴化物对酰亚胺的霍夫曼型重排的影响.
摘要:使用kbr作为催化剂的芳族和脂族酰亚胺的霍夫曼型重排进行以提供芳族和脂族氨基酸衍生物.我们还开发了这种方法合成加巴喷丁的新合成途径.
DOI:10.1039/c2Cc33914E

专利信息

专利号:US-11987826-B2
优先权日:2020-01-21
标 题:Nitrilase mutant and application thereof in the synthesis of an anti-epileptic drug intermediate
发明人：XUE YAPING; XIONG NENG; Lv Peijin; ZHENG YUGUO
权利人:UNIV ZHEJIANG TECHNOLOGY
摘要:The present invention provides a nitrilase mutant protein with increased thermal stability and its application in the synthesis of an anti-epileptic drug intermediate, wherein the mutant is obtained by mutating one or two of the amino acids at position 151, 223 and 250 of the amino acid sequence shown in SEQ ID No. 2. the thermal stability of the nitrilase mutant AcN-T151V/C223A/C250G was increased by up to 1.73 folds. The yield of the final product was up to 95% using the recombinant Escherichia coli containing the nitrilase mutant to hydrolyze 1M 1-cyanocyclohexylacetonitrile to produce 1-cyanocyclohexyl acetic acid at 35° C. And the yield of the final product was up to 97% when hydrolyzing 1.2M 1-cyanocyclohexylacetonitrile at 35° C. The final yield was up to 80% when using the nitrilase mutants obtained by the present invention to synthesize gabapentin.

专利号:US-7423169-B2
优先权日:2001-06-11
标 题:Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
发明人：RAILLARD STEPHEN P; ZHOU CINDY X; YAO FENMEI; MANTHATI SURESH KUMAR; XIANG JIA-NING; GALLOP MARK A
权利人:XENOPORT INC
摘要:The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.

专利号:US-11807883-B2
优先权日:2020-11-03
标 题:Polypeptide tag, highly soluble recombinant nitrilase and application thereof in synthesis of pharmaceutical chemicals
发明人：XUE YAPING; XIE DONG; XIONG NENG; ZHENG YUGUO
权利人:UNIV ZHEJIANG TECHNOLOGY
摘要:The present invention provides a polypeptide tag and its application in the synthesis of pharmaceutical chemicals, the recombinant nitrilase was obtained by connecting a polypeptide tag to the N-terminus of the amino acid sequence of the nitrilase; wherein amino acids at both ends of the polypeptide tag are uncharged glycine G, and the rest are a random combination of any one or more of glycine G, histidine H, glutamic acid E, aspartic acid D, lysine K and arginine R; The activity of the recombinant nitrilase in the preparation of 1-cyanocyclohexyl acetic acid is up to 3034.7 U/g dcw, the polypeptide tag significantly improves the soluble expression of nitrilase, and the whole cell catalyst hydrolyzes 1M substrate with the same concentration 30 minutes faster than the mother enzyme. The method provided by the present invention can also be used for the biocatalytic reaction of other pharmaceutical intermediates as the substrate catalyzed by the nitrilase, improving the activity of the whole cell catalyst in reaction, and also improving the solubility of other types of nitrilases and the activity of the corresponding whole cell catalysts.

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-6765114-B1
优先权日:1998-12-29
标题 :Process for the synthesis of 1-(aminomethyl)cyclohexyl-acetic acid
发明人：GIZUR TIBOR; LENGYEL ZOLTANNE; SZALAI KRISZTINA
权利人:RICHTER GEDEON VEGYESZET
摘要:The invention relates to a new process for the synthesis of 1-(aminomethyl)cyclohexyl-acetic acid of formula (I) via the new intermedier 1-(nitromethyl)cyclohexyl-acetic acid derivative of formula (II), wherein R represents hydrogen, benzyl group, diphenylmethyl group or C 1 -C 4 alkyl or alkoxy aromatic ring substituted derivatives thereof.

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.