CAJ | 학술논문

2-氯吡啶经氧化、亲核取代、Pd/C催化氢化得3-(吡啶-2-基氨基)丙酸乙酯(2).另用对氯甲苯经氧化、硝化、胺化、酰氯化制得4-甲胺基-3-硝基苯甲酰氯(3).2和3缩合得3-[(4-甲胺基-3-硝基苯甲酰基)(吡啶-2-基)氨基]丙酸乙酯(4),再经催化氢化还原、酰胺化后闭环、成脒及酰化反应等制得抗凝血药达比加群酯,总收率约12%(以对氯甲苯计).
2-록필정경양화、친핵취대、Pd/C최화경화득3-(필정-2-기안기)병산을지(2).령용대록갑분경양화、초화、알화、선록화제득4-갑알기-3-초기분갑선록(3).2화3축합득3-[(4-갑알기-3-초기분갑선기)(필정-2-기)안기]병산을지(4),재경최화경화환원、선알화후폐배、성미급선화반응등제득항응혈약체비가군지,총수솔약12%(이대록갑분계).
3-(Pyridin-2-ylamino)propinoie acid ethyl ester(2)was prepared from 2-chloropyridine by oxidation,substitution and then hydrogenation.4-Methylamino-3-nitrobenzoyl chloride(3)was prepared from 4-chlorotoluene by oxidation,nitration,amination and chlorination.Dabigatran etexilate was synthesized from 2 and 3 by condensation,reduction,amidation,cyclization,amidination and acylation with an overall yield of about 12%(based on 4-chlorotoluene).