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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1509518Generated: October 31, 2026

1,5-Pentanediol → HCID 58355233, compound

https://huagongshe.com/reaction/1509518

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1,5-PentanediolHCID 8105—
ReactantTriphenylphosphineHCID 11776—
ReactantDiisopropyl diazene-1,2-dicarboxylateHCID 75555—
Reactanttert-Butyl (3S,5R)-3-{(1H-benzimidazol-2-ylcarbonyl)(2-methylpropyl)amino)-5-(morpholin-4-ylcarbonyl)piperidine-1-carboxylateHCID 58355717—
SolventTolueneHCID 1140—
SolventTetrahydrofuranHCID 8028—
SolventSodium BicarbonateHCID 516892—
ProductHCID 58355233HCID 5835523369.5%

Reaction Steps

To a mixed solution of tert-butyl (3S,5R)-3-[(1H-benzimidazol-2-ylcarbonyl)(2-methylpropyl)amino]-5-(morpholin-4-ylcarbonyl)piperidine-1-carboxylate (308 mg), pentane-1,5-diol (1.25 g) and triphenylphosphine (472 mg) in toluene (10 ml)-THF (10 ml) was added diisopropyl azodicarboxylate (910 μl) at room temperature, and the mixture was stirred at the same temperature for 15 hr. The reaction mixture was diluted with aqueous sodium bicarbonate, and the mixture was extracted with ethyl acetate. The extract was washed with saturated brine, and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure. The residue was subjected to silica gel column chromatography, and a fraction eluted with ethyl acetate was concentrated under reduced pressure to give the object product (250 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09221836B2
Source datasetuspto-grants-2015_12
ORD IDord-580b7090bed8491aa8bc83b680516dda
Source noteuspto-grants-2015_12