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以3-氨基-1-[3-(环己基甲氧基)苯基]丙-1-醇为原料,经氨基保护、氧化、手性还原、脱保护和成盐等5步反应合成了Emixustat,总收率30.7%,其结构经1H NMR和MS(ESI)确证。 相似文献
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Using arteannuin B (2) isolated from Artemisia annua L.,a number of chemical transformations have been carried out, i.e., catalytic hydrogenation of 2 to give a mixture of 5, 6 and 7, reaction of 6 with boron trifluoride etherate to give 8 and 9, saponification of 6 with potassium hydroxide and deoxygenation of 2, 6 and 7 with iron pentacarbonyl to give 18, 4 and 3, respectively. 相似文献
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Arteannuin (1), a new sesquiterpene lactone containing a peroxide group, is the antimalarial active principle isolated from Artemisia annua L. Deoxyarteannuin (2) occurs in the same plant and was isolated as a metabolite from the urine of patients treated with arteannuin. We now report a stereocontrolled synthesis of these two naturally occurring sesquiterpene lactones starting from arteannuic acid (5) by the reaction sequence as shown in Scheme 2 (see Chinese Text). Irradiation of the methanolic solution of the key intermediate 3 in the resence of oxygen and a sensitizer (Rose Bangal) with 200 W high pressure mercury lamp followed by acid treatment gave 1 in 28% yield (2 steps), m.p. 151-153`c, 相似文献
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