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(R,R)-福莫特罗关键中间体的合成研究 被引量：1

Synthesis of the Key intermediate for(R,R)-formoterol
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摘要 以4-苄氧-3-硝基苯乙酮为原料,经溴代、不对称还原、选择性还原硝基和甲酰化,合成(R,R)-福莫特罗关键中间体(母核)(R)-N-[2-苄氧基-5-(2-溴-1-羟乙基)苯基]甲酰胺(2),为进一步研究开发奠定基础.目标化合物的结构经IR1、HNMR、MS等确证,4步收率达41%. （ R ）-N- [ 2- （benzyloxy） -5- （2-bromo-1-hydroxyethyl ） phenyl ] formamide （ 2 ）, the key intermediate of （R, R ）-formoterol, was synthesized starting from 4-benyloxy-3-nitroate phenone via bromination, asymmetric reduction, selective reduction of nitro group and formylation. The proposed method is feasible to synthesize the title compound and is suitable for large-scale preparation. The chemical structure of the target compound was confirmed by IR, 1^HNMR and MS. The title compound was obtained in 41% overall yield.
作者 崔香娟 吴勇 陈瑶瑶 陈雷 海俐
机构地区 四川大学华西药学院
出处 《四川大学学报（自然科学版）》 CAS CSCD 北大核心 2008年第3期628-630,共3页 Journal of Sichuan University(Natural Science Edition)
关键词 (R R)-福莫特罗 (R)-N-[2-苄氧基-5-(2-溴-1-羟乙基)苯基]甲酰胺 合成 （ R, R ）-Formaterol, （ R ）-N- [ 2- （ benzyloxy）-5- （2-bromo-l-hydroxyethyl） phenyl ] formamide, synthesis
分类号 R978 [医药卫生—药品]
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参考文献5

  • 1Gunar A, John M. Aerosol formulations contatining micronized optically pure (R, R )- formoterol for bronchodilating therapy; US, 6299863 [P]. 2001.
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同被引文献14

  • 1Murase K, Mase T, Ida H, et al. Absolute configurations of four isomers of 3-formamido-4-hydroxy-c [ [N- (p-methoxy- c-methylphenethyl) amino] methyl] benzyl alcohol, a potent ~-adrenoreceptor stimulant [J]. Chem Pharm Bull, 1978, 26(4): 1123-1129.
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四川大学学报（自然科学版）
2008年 第3期

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