Synthesis method for preparing artemisinin
A technology for the synthesis of artemisinin and artemisinin, which is applied in the field of synthetic artemisinin preparation, can solve the problems of small toxic and side effects, damage to the environment and ecological balance, time-consuming and labor-intensive problems, and achieve reasonable and simple design, easy industrial application, and reduce manufacturing costs. cost effect
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[0030] 1) Synthesis of Compound 2
[0031] Using cyclohexenone (26g, 260mmol) as the starting material, add dimethyl zinc, copper trifluoromethanesulfonate (0.96g, 2.6mmol), phosphoramidite (2.6g, 5.2mmol), benzene (500ml) The reaction was carried out under stirring at -30°C-RT for 12 hours. The biphenylphosphonamidite formed by benzene and phosphoramidite was used as a ligand, and copper trifluoromethanesulfonate was used as a catalyst to catalyze the reaction of dimethyl zinc on cyclohexenone. Conjugate addition, then add crotyl bromide (38.6g, 286mmol), carry out the alkylation to crotyl bromide, obtain compound 2 (27g, 157mmol) with 61% yield, the trans isomerization of the compound 2 The ratio to cis isomerism, ie trans-cis=7:1, and the target product content is 91%.
[0032] 2) Synthesis of compound 3
[0033] After adding compound 2 (27g, 157mmol) and tosylhydrazide (230g, 157mmol), MeOH (100ml) mixed, stirred at room temperature for 12h, the reaction can get the corr...
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