CAS: 361442-00-4; (2S)-2-((Tert-Butoxycarbonyl)Amino)-2-(3-Hydroxyadamantan-1-yl)Acetic Acid

上下游产品

CAS号361441-97-6 N-叔丁氧羰基-L-金刚烷基甘氨酸 | CAS号361441-95-4 1-(S)-adamantan... | CAS号2094-74-8 1-金刚烷甲醛 | CAS号770-71-8 1-金刚烷甲醇 | CAS号828-51-3 1-金刚烷甲酸 | CAS号711-01-3 1-金刚烷甲酸甲酯 | CAS号95853-35-3 (2S)-2-(1-adama... | CAS号1334321-39-9 (R)-N-B°C-3-羟基金... | CAS号102502-64-7 (S)-2-(金刚烷-1-基)... | CAS号361442-01-5 沙格列汀中间体6 | CAS号709031-43-6 N-[(1S)-2-[(1S,...

1-金刚烷甲酸置于盐酸,Potassium Permanganate,氯化亚砜,Nickel Aluminum,(1R,2S)-2-氨基-1,2-二苯基乙醇,盐酸羟胺,苄基三乙基氯化铵,Sodium,Potassium Hydroxide,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,水,乙酸乙酯,Petroleum Ether,叔丁醇 作为反应溶剂,化学反应 27.0H,反应生成 N-叔丁氧羰基-3-羟基-1-金刚烷基-D-甘氨酸
参考文献:(S)-N-Boc-3-Hydroxyadamantylglycine合成的便捷方法:沙格列汀的关键中间体
标题:(S)-N-Boc-3-Hydroxyadamantylglycine合成的便捷方法:沙格列汀的关键中间体
摘要:(S)-N-Boc-3-羟基金刚烷基甘氨酸是沙格列汀的关键中间体.由1-金刚烷羧酸合成得到1-乙酰金刚烷(2),将其通过氧化转化为2-(1-金刚烷基)-2-氧乙酸(3),然后转化为1-金刚烷基-2-羟基亚氨基乙酸.酸(4),然后处理盐酸羟胺,然后将4还原并进行boc保护,得到n-Boc-金刚烷基甘氨酸(5),将其用kmno4氧化并用手性碱处理.利用该途径,制备了(S)-N-Boc-3-羟基金刚烷基甘氨酸.这项工作是阐述合成(S)-N-Boc-3-羟基金刚烷基甘氨酸的简便途径,并为合成沙格列汀提供新的思路.
DOI:10.2174/1570178611666140421231237

专利信息

专利号:US-2016107992-A1
优先权日:2013-06-20
标 题:Intermediates useful for the preparation of saxagliptin
发明人：CASTALDI GRAZIANO; PALLANZA GIUSEPPE; GABOARDI MAURO; CASTALDI MARTA
权利人:CHEMELECTIVA S R L
摘要:Intermediates useful for the synthesis of saxagliptin and their preparationare described.

专利号:WO-2014057495-A1
优先权日:2012-10-11
标 题 :A process for industrial preparation of [(s)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine
发明人：ALLA VENKAT REDDY; ALLA RAGHU MITRA; DUBEY AJAY KUMAR; REDDY P RAMAKRISHNA
权利人:LEE PHARMA LTD; ALLA VENKAT REDDY; ALLA RAGHU MITRA; DUBEY AJAY KUMAR; REDDY P RAMAKRISHNA
摘要:A commercially viable process for industrial preparation of [(S)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine which is a key intermediate for saxagliptin synthesis and is represented by compound of Formula-VI. The compound-VI obtained by the process of present invention has more than 99.5% HPLC purity, not more than 0.15 % of dihydroxy impurity, not more than 0.05% of isomer impurity and not more than 0.1% of any unknown impurity. Formula (VI).

专利号:US-9150511-B2
优先权日:2011-05-24
标题 :Process for preparing saxagliptin and its novel intermediates useful in the synthesis thereof
发明人：KOVI RAVISHANKER; RAPOLE KESHAVRAO; NAIK ASHISH; KANNAPAN JAYARAMAN; MADALA MURALIKRISHNA; THAKOR SANJAY
权利人:APICORE US LLC
摘要:Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.