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4-(2-溴乙酰基)-3-氟苯硼酸的制备 被引量:2

Preparation of 4-(2-Bromoacetyl)-3-fluorophenylboronic Acid
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摘要 4-溴-2-氟苯基氰经格氏反应得到4-溴-2-氟苯乙酮,先保护羰基,再经格氏反应和二羟硼基取代、溴代制得4-(2-溴乙酰基)-3-氟苯硼酸,总收率54%。 4-(2-Bromoacetyl)-3-fluorophenylboronic acid was synthesized from 4-bromo-2-fluorobenzonitrile by Grignard reaction, protection of carbonyl with ethanediol, Grignard reaction and substitution by borono group to give 4-acetyl-3-fluorophenylboric acid followed by bromination with an overall yield of 54%.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2005年第9期533-534,共2页 Chinese Journal of Pharmaceuticals
关键词 4-(2-溴乙酰基)-3-氟苯硼酸 中间体 合成 4-(2-bromoacetyl)-3-fluorophenylboronic acid intermediate synthesis
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参考文献2

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  • 2Farley H, Randall S, Mandeville W, et al. Preparation of aryl boronic acids for treating obesity [P]. WO: 2003002570,2003-01-09. (CA 2003, 138: 73376).

同被引文献14

  • 1陈绪胄,李建平.辣根过氧化酶在纳米银修饰玻碳电极上的直接电化学研究[J].传感技术学报,2007,20(11):2373-2376. 被引量:14
  • 2李英奇,伍佑华,彭雨春.芳基硼酸在有机合成中的应用[J].精细化工中间体,2006,36(1):14-17. 被引量:17
  • 3Trenkle W C, Barkin J L, Son U S, et tl. Highly efficient 1,4 additions of electron-deficient ary/ boronic acids wilh a novel Rhodium(D quinonoid catalyst [J ]. Organometallics, 2006, 25(15) :3548 -3551.
  • 4Ishihara K, Ohara S, Yamamoto H. Direct polycondensation of carboxylic acids and amines catalyzed by 3,4,5 trifluoro phenylboronic acid[J]. Macromolecules, 2000, 33 (10): 3511-3513.
  • 5KD巴恩斯.制备5-溴-2-氟苯硼酸的方法:CN,1403430A[P].2003-03-19.
  • 6TSUTOMU F, EI-ICHI S KOZUE S, et al. Palladium-catalyzed cross-coupling of N-benzenesulfonyl-3,4-dibromopyrrole and its application to the total syntheses of lamellarins O, P, Q, and R[J]. Tetrahedron, 2008, 64(2):328-338.
  • 7LI W, DORIAN P ,MARK S, et al. An improved Protocol for the preparation of 3-Pyridyl- and some arylboronic acids [J].The Journal of Organic Chemistry, 2002, 67( 15 ):5394-5397.
  • 8FROHN H J, ADONIN N Y, BARDIN V V, et al. Polyfluoroorga- noboron-Oxygen Compounds( 1 ) Polyfluorlnated Aryl(dihydroxy) boranes and Tri(aryl) boroxins[J]. Z. Anorg. Allg. Chem, 2002, 628 ( 13):2827 -2833.
  • 9邓鹏,薛文通,宋康,王文亮.循环伏安法测定油脂中过氧化物含量的研究[J].中国食物与营养,2008,14(4):26-29. 被引量:4
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