CAJ | 학술논문

N-(叔丁氧羰基)-L-谷氨酰胺(2)经分子内环合、脱保护得中间体3-氨基-2,6-哌啶二酮三氟乙酸盐(4);另用2-甲基-3-硝基苯甲酸甲酯(5)经溴化制得另一中间体2-溴甲基-3-硝基苯甲酸甲酯(6).4与6经缩合、还原制得来那度胺,总收率约33%(以5计).
N-(숙정양탄기)-L-곡안선알(2)경분자내배합、탈보호득중간체3-안기-2,6-고정이동삼불을산염(4);령용2-갑기-3-초기분갑산갑지(5)경추화제득령일중간체2-추갑기-3-초기분갑산갑지(6).4여6경축합、환원제득래나도알,총수솔약33%(이5계).
N-Boc-L-glutamine (2) was subjected to intramolecular cyclization and deprotection to give the intermediate 3-amino-2,6-piperidinedione trifluoroacetate (4). The other intermediate methyl 2-bromomethyl-3-nitrobenzoate (6) was obtained from 2-methyl-3-nitrobenzoic acid methyl ester(5)via bromination. Compound 4 and 6 underwent condensation, followed by reduction to give lenalidomide with an overall yield of about 33% (based on compound 5).