Synthesis method of deuterium or tritium labeled docetaxel
The invention discloses a preparation method of deuterium or tritium labeled docetaxel, which comprises the following steps: (1) under the action of organic alkali, carrying out esterification reaction on deuterium or tritiated tert-butyl alcohol and p-nitrophenyl chloroformate to obtain deuterium o...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a preparation method of deuterium or tritium labeled docetaxel, which comprises the following steps: (1) under the action of organic alkali, carrying out esterification reaction on deuterium or tritiated tert-butyl alcohol and p-nitrophenyl chloroformate to obtain deuterium or tritiated (4-nitrophenyl) tert-butyl carbonate; and (2) carrying out amidation reaction on the deuterium or tritiated (4-nitrophenyl) tert-butyl carbonate obtained in the step (1) and a compound IM-1, and after the reaction is completed, carrying out post-treatment to obtain docetaxel, the synthesis method has the advantages of convenient intermediate synthesis, stable chemical properties, high utilization rate of the deuterated reagent and high product yield.
本发明公开了一种氘或氚标记的多西他赛的制备方法,包括以下步骤:(1)在有机碱的作用下,氘或氚代叔丁醇和对硝基苯基氯甲酸酯进行酯化反应,得到氘或氚代(4-硝基苯基)碳酸叔丁酯;(2)步骤(1)得到的氘或氚代(4-硝基苯基)碳酸叔丁酯与化合物IM-1进行酰胺化反应,反应完成后经过后处理得到所述的多西他赛;该合成方法中间体合成方便,化学性质稳定,并且氘代试剂的利用率和产物收率高。 |
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