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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 490805Generated: October 30, 2026

1-Hydroxybenzotriazole → 1-(1-{2-[Cis-2,5-dipropylpyrrolidin-1-yl]-2-oxoethyl}-6-methoxy-1H-indazol-3-yl)-2,2-dimethylpropan-1-one

https://huagongshe.com/reaction/490805

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1-HydroxybenzotriazoleHCID 75771—
ReactantDiisopropylethylamineHCID 81531—
Reactant(2R,5S)-2,5-DipropylpyrrolidineHCID 14564783—
Reactant[3-(2,2-Dimethylpropanoyl)-6-methoxy-1H-indazol-1-yl]acetic acidHCID 57675531—
Solvent1,2-DichloroethaneHCID 11—
SolventDimethylformamideHCID 6228—
Product1-(1-{2-[Cis-2,5-dipropylpyrrolidin-1-yl]-2-oxoethyl}-6-methoxy-1H-indazol-3-yl)-2,2-dimethylpropan-1-oneHCID 10025563—

Reaction Steps

To a solution of 28.3 mg [3-(2,2-dimethylpropanoyl)-6-methoxy-1H-indazol-1-yl]acetic acid from the Step E Example 44 in 1 mL DMF was added 23.0 mg HOBt, 23.3 mg cis-2,5-dipropylpyrrolidine from the Step A above, 38.3 mg EDC, and 45.2 mg DIEA in that order. The mixture was stirred at room temperature over night and purified by RP-HPLC using 70-100% MeCN gradient. The pure product fractions were pooled and lyophilized to give the title compound as white solid. LC-MS: 4.50 min. (m/Z=428.4, 450.3).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07528163B2
Source datasetuspto-grants-2009_05
ORD IDord-8ed9d08e89054625850d67c05e7e660f
Source noteuspto-grants-2009_05