知识与财富的链接
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.
