3_2_氯_6_氟苯基_5_甲基_4_异恶唑甲酰氯的合成_陈志卫.pdf

3-( 2--6-)-5--4- * 陈志卫, 闫伟华, 苏为科 (, 310014) : 研究抗生素氟氯西林钠的关键中间体 3-( 2-氯-6-氟苯基)-5-甲基-4-异噁唑甲 氯的合成方法, 使之适合工业化 生产 以 2-氯-6-氟苯甲醛为原料, 经肟化氯化环合水解 氯化等步骤制得目标化合物 合成产物的化学 1 13 结构经 IR, H-NMR, C-NMR an MS确证, 总收率为 60. 2% 此方法收率高, 成本低, 适合工业化生产 : 氟氯西林钠; 3-( 2-氯-6-氟苯基)-5-甲基-4-异噁唑甲 氯; 合成 : R916. 693 : A : 1007-7693( 2008) 04-0308-02 Synthesis of 3-(2-Chloro-6-fluorophenyl)-5-m ethylisoxazole-4-carbonyl Chloride * CHEN Zhi-w e,i YAN W e-i hua, SU W ei-ke ( Colleg e of P harmaceut ical Sc iences, Zhej iang Un iv er sity of Technology, H angzhou 310014, Ch ina) A STRACT: O JECTIVE To stu y the synthetic metho of 3-( 2-Ch loro-6-fluoro phenyl)-5-m ethylisoxazole-4-carbonyl ch lori e. METHODS The objective compoun was synthesize by steps of oxmi ation, chlorination, cyclization, hy rolysis, acyl ch lorination, 1 starting from 2-ch loro-6-fluorobenzal ehy e. RESULTS The chem ical structure of synthetic pro ucts w as confirm e by IR, H- NMR, 13 C-NMR an MS, the total yiel was am ount to 60. 2% . CONCLUSION Th is synthetic route is practicalw ith h igh yiel an low cost. KEY WORDS: Flucloxacillin; 3-( 2-Chloro-6-fluorophenyl)-5-m ethylisoxazole-4-carbonyl chlori e; synthesis 3-( 2--6-)-5--4-( 4) 5--4-( 3) N aOH , , , [ 1] , NaOH , , , [ 2-5] , 2--6-, 65. 5% 3-( 2--6- )-5--4- [2] (4) , [ 1] : , 2--6-( 2)