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5-硝基水杨醛与氯乙基吡咯烷盐酸盐经亲核取代得到5-硝基-2-[2-(吡咯烷-1-基)乙氧基]苯甲醛,然后经醛基还原、取代、硝基还原及成盐得到3-[(烯丙氧基)甲基]-4-[2-(吡咯烷-1-基)乙氧基]苯胺二对甲苯磺酸盐,接着与4-[3-[(烯丙氧基)甲基]苯基]-2-氯嘧啶缩合得到N-[3-[(烯丙氧基)甲基]-4-[2-(吡咯烷-1-基)乙氧基]苯基]-4-[3-[(烯丙氧基)甲基]苯基]嘧啶-2-胺,最后经烯烃复分解反应得到pacritinib盐酸盐,总收率约13%(以5-硝基水杨醛计)。
Nucleophilic substitution of 5-nitrosalicylaldehyde with chloroethylpyrrolidine hydrochloride gives 5-nitro-2- [2- (pyrrolidin-1-yl) ethoxy] benzaldehyde, Reduction, substitution, reduction with a nitro group and salt formation gives the 3 - [(allyloxy) methyl] -4- [2- (pyrrolidin- 1 -yl) ethoxy] aniline di-p-toluenesulfonate followed by Is condensed with 4- [3 - [(allyloxy) methyl] phenyl] -2-chloropyrimidine to give N- [3 - [(allyloxy) methyl] -4- [2- Yl] ethoxy] phenyl] -4- [3 - [(allyloxy) methyl] phenyl] pyrimidin-2-amine, finally paclitinib hydrochloride was obtained by olefin metathesis reaction, Rate of about 13% (5-nitrosalicylaldehyde count).