摘要
N-(叔丁氧羰基)-L-谷氨酰胺(2)经闭环、脱保护制得3-氨基-2,6-哌啶二酮三氟乙酸盐(4)。另用3-硝基邻苯二甲酸(5)脱水制得3-硝基邻苯二甲酸酐(6)。4和6经缩合、铁粉/浓盐酸还原制得免疫调节剂类抗肿瘤药3-氨基-N-(2,6-二氧代-3-哌啶基)-邻苯二甲酰亚胺,以5计总收率约35%。
Pomalidomide, an immunomodulator, was synthesized from 3-nitrophthalic acid (5) by dehydration to give 3-nitrophthalic anhydride (6), which was subjected to the reaction with 3-aminopiperidine-2,6-dione trifluoroacetate (4) to afford 3-nitro-N-(2,6-dioxopiperidin-3-yl)-phthalimide (7) followed by reduction with Fe/HCl in an overall yield of about 35 % ( based on compound 5). Compound 4 was prepared from N-Boc-L-glutamine by cyclization and deprotection.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2009年第10期721-723,共3页
Chinese Journal of Pharmaceuticals