참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Hippuric Acid | HCID 464 | — |
| 반응물 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 반응물 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 반응물 | 1-(4-Chlorobenzyl)pyrrolidin-3-amine dihydrochloride | HCID 18426180 | — |
| 용매 | Chloroform | HCID 6212 | — |
| 용매 | Triethylamine | HCID 8471 | — |
| 생성물 | 3-(N-benzoylglycyl)amino-1-(4-chlorobenzyl)pyrrolidine | HCID 9842404 | 95.2% |
반응 단계
N-Benzoylglycine (9.3 mg, 0.055 mmol), 3-ethyl-1-[3-(dimethylamino)propyl]carbodiimide hydrochloride (EDCI) (1.05 mg) and 1-hydroxybenzotriazole hydrate (HOBt) (7.4 mg) were added to a chloroform (2.5 mL) solution of 3-amino-1-(4-chlorobenzyl)pyrrolidine dihydrochloride (14.2 mg, 0.050 mmol) and triethylamine (15.2 mg). The resulting reaction mixture was stirred at 25° C. for 16 hours and then washed with a 2 M aqueous solution of NaOH (2 mL×2) and brine. After filtration through a PTFE membrane filter, the solvent was removed under reduced pressure to provide 3-(N-benzoylglycyl)amino-1-(4-chlorobenzyl)pyrrolidine (Compd. No. 1) as an off-white oil (17.7 mg, 95%). The purity was determined by RPLC/MS (95%). ESI/MS m/e 372.0 (M++H, C20H22ClN3O2).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US07390830B1 |
|---|
| 출처 데이터셋 | uspto-grants-2008_06 |
|---|
| ORD ID | ord-72cd6b5d7b994755b2e85d03e19ae34e |
|---|
| 출처 메모 | uspto-grants-2008_06 |
|---|
