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N-Boc-4-羟基哌啶经酯化、亲核取代、脱保护、芳构化反应得4-[4-(4-三氟甲氧基苯氧基)哌啶-1-基]苯酚(6);?-甲基烯丙醇经Sharpless不对称环氧化、对硝基苯磺酰氯活化得关键中间体(R)-4-硝基苯磺酸-2-甲基缩水甘油酯(9);6和9经亲核取代、环合得治疗耐多药肺结核病药物地依麦迪,总收率约30%(以?-甲基烯丙醇计),纯度99.9%,ee值达100%。
N-Boc-4-hydroxypiperidine is esterified, nucleophilic substituted, deprotected and aromatized to give 4- [4- (4- trifluoromethoxyphenoxy) piperidin-1-yl] phenol (6);? - methallyl alcohol by Sharpless asymmetric epoxidation, p-nitrobenzenesulfonyl chloride activation of the key intermediate (R) -4-nitrobenzene sulfonate 2-methyl glycidyl ester 9); 6 and 9 nucleophilic substitution, cyclodextrine treatment of multi-drug resistant tuberculosis drug to McGrady, the total yield of about 30% (with? - Methalyl alcohol dollars), purity 99.9%, ee value 100%.