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ChemicalBook CAS DataBase List Eribulin intermediate

Eribulin intermediate synthesis

2synthesis methods
7,11:10,14:13,16:21,24:27,31-Pentaepoxy-2H-cyclohentriaconta[b]furan-5,18(3H,4H)-dione, 2-[(2S)-2,3-dihydroxypropyl]octacosahydro-12,15-dihydroxy-3-methoxy-29-methyl-23,30-bis(methylene)-, (2R,3R,3aS,7R,10S,11R,12S,13S,14S,15S,16R,21S,24S,27S,29R,31R,32aS)- (9CI)

728043-99-0
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Eribulin intermediate

253128-15-3
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Yield:253128-15-3 93 %

Reaction Conditions:

with pyridinium p-toluenesulfonate in dichloromethane;Inert atmosphere;

Steps:

5

Dissolve the obtained E-29-4 in 1.3L of dichloromethane, add 120g of pyridinium 4-methylbenzenesulfonate, stir and react for 2h under the protection of nitrogen, and directly spin evaporate the reaction to obtain the crude product of E-30-4 , 55.1 g of pure E-30-4 was obtained by column chromatography, the total yield from E28a to E-30-4 was 93%, and the purity was 96%.

References:

CN115197239,2022,A Location in patent:Paragraph 0108-0112

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