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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 40094Generated: October 26, 2026

Phosphorus oxide (P4O10) → 6-(5,5-Dimethyl-4,5-dihydrooxazol-2-yl)-N-(4-fluorobenzyl)-2-isopropyl-1-(pyridin-2-ylmethyl)-1H-indole-3-carboxamide

https://huagongshe.com/reaction/40094

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPhosphorus oxide (P4O10)HCID 14812—
Reactant1-Benzyl-N3-(3,4-difluorobenzyl)-N6-(2-hydroxy-2-methylpropyl)-2-isopropyl-1H-indole-3,6-dicarboxamideHCID 69226164—
ReactantN3-(4-fluorobenzyl)-N6-(2-hydroxy-2-methylpropyl)-2-isopropyl-1-(pyridin-2-ylmethyl)-1H-indole-3,6-dicarboxamideHCID 69227964—
SolventBenzeneHCID 241—
Product6-(5,5-Dimethyl-4,5-dihydrooxazol-2-yl)-N-(4-fluorobenzyl)-2-isopropyl-1-(pyridin-2-ylmethyl)-1H-indole-3-carboxamideHCID 69227909—

Reaction Conditions

Temperature50 °C

Reaction Steps

To a solution of N3-(4-fluorobenzyl)-N6-(2-hydroxy-2-methylpropyl)-2-isopropyl-1-(pyridin-2-ylmethyl)-1H-indole-3,6-dicarboxamide (Compound 68, 23 mg, 0.043 mmol) in benzene (6 ml) at 25° C. was added P2O5 (120 mg, 0.86 mmol). The mixture was stirred at 50° C. for 4 h, quenched with 6N NaOH (1 ml), extracted several times with EtOAc, washed with H2O, brine, dried over Na2SO4, concentrated in vacuo. The residue was purified by chromatography on silica gel (100% EtOAc) to yield the title compound as yellow oil.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08524917B2
Source datasetuspto-grants-2013_09
ORD IDord-f16ce2aadef3440c99be1112c3cf515b
Source noteuspto-grants-2013_09