CAS: 623950-02-7; (S)-2-((Tert-Butoxycarbonyl)Amino)-3-(4-Carbamoyl-2,6-Dimethylphenyl)Propanoic Acid

相似化合物

623950-05-0 1870867-59-6 943449-15-8

上下游产品

methyl (S)-2-((tert-butoxycarbonyl)amino)-3-(4-carbamoyl-2,6-dimethylphenyl)propanoate 4'-carboxyl N-B°C-2',6'-dimethyl-L-phenylalanine methyl ester methyl (S)-2-((tert-butoxycarbonyl)amino)-3-(2,6-dimethyl-4-(((trifluoromethyl)sulfonyl)oxy)phenyl)propanoate methyl (S)-2-((tert-butoxycarbonyl)amino)-3-(4-hydroxy-2,6-dimethylphenyl)propanoate {1-(4-carbamoyl-2,6-dimethyl-benzyl)-2-oxo-2-[2-(4-phenyl-1H-imidazol-2-yl)-piperidin-1-yl]-ethyl}-carbamic acid tert-butyl ester {1-(4-carbamoyl-2,6-dimethyl-benzyl)-2-oxo-2-[3-(4-phenyl-1H-imidazol-2-yl)-3,4-dihydro-1H-isoquinolin-2-yl]-ethyl}-carbamic acid tert-butyl ester

(S)-2-Tert-Butoxycarbonylamino-3-(4-Methoxycarbonyl-2,6-Dimethylphenyl)Propionic Acid置于n-甲基吡咯烷酮,Sodium Methylate,Formamide体系中,用 甲醇 作为反应溶剂,化学反应 1.0H,以69%的收率获得产物叔丁氧羰基-2,6-二甲基-4-甲酰胺基-L-苯丙氨酸
参考文献:艾沙度林中间体的制备方法
标题:艾沙度林中间体的制备方法
摘要:本发明提供了一种艾沙度林中间体的制备方法,具体公开了制备下式11所示(S)‑2‑叔丁氧羰基氨基‑3‑(4‑氨甲酰基‑2,6‑二甲基苯基)丙酸的方法,包括:步骤i,由式1所示的化合物获得式4所示的化合物;步骤ii,由式4所示的化合物获得式5所示的化合物;步骤iii,使式5所示的化合物获得式6所示的化合物;步骤iv,对式6所示的化合物中的氨基进行保护获得式9所示的化合物;和步骤v,由式9所示的化合物经选择性水解得到式10所示的化合物,然后经氨解经获得式11所示的化合物.本发明的工艺路线为全新设计,各步反应得到的中间体均为首次合成,工艺路线中采用了先羰基化后不对称还原的方法,不对称还原在工艺的较后阶段实现,有利于节省催化剂用量,降低成本.

专利信息

专利号:US-9187408-B2
优先权日:2008-10-27
标 题 :Process for the preparation of protected L-alanine derivatives
发明人：ANZALONE LUIGI; FEIBUSH PENINA; VILLANI FRANK J
权利人:JANSSEN PHARMACEUTICA NV; JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.

专利号:US-7629488-B2
优先权日:2005-03-14
标 题 :Process for the preparation of opioid modulators
发明人：CAI CHAOZHONG; HE WEI
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders.