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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1855677Generated: October 31, 2026

Water → 2-propanyl (2E)-3-[(2R,5aR,6S,7R,8aS)-6-({[dimethyl(2-methyl-2-propanyl)silyl]oxy}methyl)-7-(tetrahydro-2H-pyran-2-yloxy)-3,5a,6,7,8,8a-hexahydro-2H-cyclopenta[b]oxepin-2-yl]acrylate

https://huagongshe.com/reaction/1855677

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantEthyl AcetateHCID 8857—
Reactant1-Hydroxy-1,2-benziodoxol-3(1H)-one 1-oxideHCID 339496—
ReactantHCID 68751161HCID 68751161—
SolventDimethyl SulfoxideHCID 679—
Product2-propanyl (2E)-3-[(2R,5aR,6S,7R,8aS)-6-({[dimethyl(2-methyl-2-propanyl)silyl]oxy}methyl)-7-(tetrahydro-2H-pyran-2-yloxy)-3,5a,6,7,8,8a-hexahydro-2H-cyclopenta[b]oxepin-2-yl]acrylateHCID 86665321—

Reaction Conditions

Temperature50 °C

Reaction Steps

The compound (165 mg) produced in Example 55 was dissolved in DMSO (2 mL), a Wittig reagent (carboisopropoxymethylenetriphenylphosphorane, 218 mg) and 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX, 168 mg) were added, and the mixture was stirred at 50° C. for 5 hours. To the reaction mixture were added ethyl acetate and water, and insolubles were filtered. The filtrate was extracted with ethyl acetate, and the extract was washed with an aqueous saturated sodium bicarbonate solution and a saline, dried with anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane:ethyl acetate=97:3→80:20) to obtain a titled compound (174 mg) having the following physical property values.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08962868B2
Source datasetuspto-grants-2015_02
ORD IDord-5b6afa3baa3c40a9bb12a2b7682f28cf
Source noteuspto-grants-2015_02