本文選題：吡拉格雷鈉 + 血栓素合成酶抑制劑��； 參考：《中國醫(yī)藥工業(yè)雜志》2017年05期

【摘要】：2,3,5,6-四甲基吡嗪(2)經(jīng)間氯過氧苯甲酸氧化得2,3,5,6-四甲基吡嗪單氮氧化物(3),2反應(yīng)完全,收率93.5%;3與乙酐經(jīng)Boekelheide反應(yīng)后,再經(jīng)水解、氯化得2-氯甲基-3,5,6-三甲基吡嗪(6);6與阿魏酸乙酯(7)經(jīng)縮合反應(yīng)得(E)-3-[3-甲氧基-4-[(3,5,6-三甲基吡嗪-2-基)甲氧基]苯基]丙烯酸乙酯(8),反應(yīng)結(jié)束后加水即可析出晶體,簡化了后處理,收率98.6%。8再經(jīng)水解、成鹽得吡拉格雷鈉(1),純度99.7%,總收率34.2%(以2計)。1是作者發(fā)現(xiàn)的新一代血栓素合成酶抑制劑,目前處于Ⅱ期臨床研究階段。
[Abstract]:After oxidation with m-chloro-peroxy benzoic acid, the reaction was complete. The yield of 93. 5N ~ 3 and acetic anhydride was 93. 5% with acetic anhydride, and then hydrolyzed, and then hydrolyzed after oxidation with m-chloro-peroxy benzoic acid to give a complete reaction with trimethyl pyrazine mono _ 2 in the yield of 93. 5% with acetic anhydride. (E) -3- [3-methoxy-4- [(3-) 5-trimethylpyrazine-2-methoxy] phenyl] ethyl acrylate (8) was synthesized by the condensation reaction of 2-chloromethyl -3-methylpyrazine (6) -trimethylpyrazine (6) -trimethylpyrazine (6) with ethyl ferulate (7). The yield of 98.6.8 was then hydrolyzed to form salt to obtain piologrel sodium (1) with a purity of 99.7. The total yield of 34.2% (in 2) was a new generation of thromboxane synthase inhibitor discovered by the authors. It is in the stage of stage 鈪，

本文編號：2114011