1-取代胺甲基-7,8-二去氢-4-羟基-3,7-二甲氧基-17-甲基-9α,13α,14α-吗啡烷-6-酮的合成

Synthesis of 1-Substituted Aminomethyl-7,8-didehydro-4-hydroxy-3,7-dimethoxy-17-methylmorphinan-6-one

超声波辐射下,以盐酸青藤碱为原料,在其A环1-位碳上进行Mannich反应,合成了2个新的取代胺甲基化合物1a,1b.且由化合物1a与取代芳胺及吗啉通过胺交换反应合成了8个新的取代胺甲基化合物2a～2h.所有新化合物的结构利用IR,MS,1HNMR及NOE差谱进行了表征.

Under ultrasound irradiation, two new substituted aminomethyl derivatives of sinomenine la and lb were synthesized at C-1 in A-ring through Mannich reaction. Furthermore, eight new substituted ami- nomethyl derivatives 2a-2h have been prepared by the amine exchange reaction of the compound la with aromatic amines or morpholine. The structures of the new compounds have been characterized by IR, MS, ^1H NMR and NOE spectra.