99881-46-6Relevant articles and documents
Prepartion method of itraconazole
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Paragraph 0047; 0048; 0049; 0050, (2017/04/29)
The invention discloses a preparation method of itraconazole. Raceme-glycidol which is cheap and easy to obtain is adopted as raw materials, hydroxyls at the two ends are protected by trityl and benzyl and then esterified by 2,4-dichlorobenzene formyl chloride, then, a silylation Grignard addition reaction and a beta-silicyl alcohol elimination reaction are adopted for reducing carbonyl into carbon-carbon double bonds, iodine is adopted for performing an olefin addition reaction and a stereoselectivity ring-closure reaction, triazole replacement and debenzylation are performed, and tosyl is introduced to obtain a compound 9; the compound and a compound 10 are subjected to a condensastion reaction to obtain itraconazole; the overall synthesis process is small in pollution, easy to process, few in by-product, high in reaction selectivity and purity, environmentally friendly, low in production cost and suitable for industrial production; the defects that in the prior art, the selectivity is poor, multiple by-products are produced, the yield is low, and expensive catalysts and reagents with large environmental pollution are avoided are avoided.
A simple, mild, and regioselective method for the benzylation of carbohydrate derivatives promoted by silver carbonate
Malik, Satish,Dixit, Vaibhav A.,Bharatam, Prasad V.,Kartha, K.P. Ravindranathan
experimental part, p. 559 - 564 (2010/10/04)
A simple, mild, and regioselective method has been developed for the selective benzylation and p-methoxybenzylation of carbohydrate derivatives in high yields using Ag2CO3 as the promoter. Benzylation of base-labile substrates, for w
Magnesium bromide as a mild and efficient selective deblocking agent for isopropylidene and trityl protecting groups
Haraldsson, Gudmundur G.,Stefansson, Thorarinn,Snorrason, Halldor
, p. 824 - 826 (2007/10/03)
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