- Preparation method of 4-(E3-ethoxyl-3-oxo-1-propylene-1-yl) borophenylic acid
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The invention relates the technical field of medical intermediates, and in particular relates to a preparation method of 4-(E3-ethoxyl-3-oxo-1-propylene-1-yl) borophenylic acid. By taking 4-formylphenylboronic acid as a raw material, a Wittig-Horner reaction is performed to obtain a target product, namely 4-(E3-ethoxyl-3-oxo-1-propylene-1-yl) borophenylic acid. The yield of the 4-(E3-ethoxyl-3-oxo-1-propylene-1-yl) borophenylic acid can reach about 80%. Moreover, lithium chloride and a DBU organic reagent which are low in price and are easily available are adopted, so that a low-temperature operation is avoided; and the preparation method is mild in reaction condition, simple in post-treatment process and suitable for industrial application.
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Paragraph 0007; 0019; 0020
(2017/07/08)
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- Synthesis of phenylalanine analogs
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A straight forward synthesis of phenylalanine analogs is described. Cerium ammonium nitrate (CAN) mediated addition of azide to cinnamicester, followed by reaction with sodium acetate aff orded the α-azidocinnamate in moderate yield. Hydrogenation of α-azidocinnamate, followed by BOC, CBZ or Fmoc protection gave phenylalanine analogs. A new approach for synthesizing racemic p-boronophenylalanine analog was also explored.
- Chang, Meng-Yang,Lin, Chun-Yu,Sun, Pei-Pei
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p. 1061 - 1067
(2007/10/03)
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