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

Participants

Reaction Conditions

Reaction Steps

Dissolve a mixture of 17 mg [2-(2,2-dimethylpropanoyl)-5-methoxy-1-benzofuran-3-yl]acetic acid from the Step B Example 1 and 18.5 mg HOBt in 1 mL dry DMF. Add 13.7 mg cis-2,5-dipropylpyrrolidine from the Step A above followed by 23.0 mg EDC and 35 μL DIEA. This solution was heated at 40° C. for 2 hours. It was purified directly on RP-HPLC using 70-100% MeCN gradient. The fractions containing pure product were pooled and lyophilized to give the title compound. LC-MS: 4.59 min. (m/Z=428.3, 344.2, 450.3).

Provenance & Evidence