【摘要】 用胸腺嘧啶脱氧核苷为原料,5’-位伯羟基用三苯甲基氯成醚保护,在DEAD/Ph3P作用下得到2,3’-脱水-5’-O-(三苯甲基)胸腺嘧啶脱氧核苷后,与LiN3进行叠氮化、脱保护基后用异丁醇提取得到抗病毒药齐多夫定,总收率63%。更多还原

【Abstract】 Zidovudine was synthesized from thymidine by protection of primary hydroxyl group with Ph3CCl and then converted with diethyl azodicarboxylate(DEAD) and triphenylphosphine into 2,3’-anhydro-5’-O-(trityl)thymidine, which subjected to azidation with LiN3 and then deprotection followed by isobutanol extraction in an overall yield of 63%.更多还原