反应详情

1-[3-Dimethylaminopropyl]-3-ethylcarbodiimide hydrochloride (797 mg), hydroxybenzo-triazole trihydrate (475 mg) and triethylamine (0.890 ml) were added to a stirred solution of 2-pyrrolidinyl acetic acid hydrochloride (528 mg) in dry dimethylformamide at room temperature. After 30 minutes a solution of the compound of Example 14 (800 mg) in dry dimethylformamide was added, followed by triethylamine (0.590 ml). The resulting solution was stirred at room temperature for 4 hours. The reaction was quenched with water and extracted into diethyl ether then the organic solution was dried (MgSO4) and evaporated to give a yellow oil. The residue was purified by chromatography on grade 3 neutral alumina (1% methanol/dichloromethane) then treated with ethereal hydrogen chloride to afford the title compound, mp=106°-108° C.;

1. customThe reaction was quenched with water
2. extractionextracted into diethyl ether
3. dry with materialthe organic solution was dried (MgSO4)
4. customevaporated
5. customto give a yellow oil
6. customThe residue was purified by chromatography on grade 3 neutral alumina (1% methanol/dichloromethane)
7. additionthen treated with ethereal hydrogen chloride