Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 917303생성일: 2026년 10월 25일
Dimethylformamide → Benzo[b]thiophene-2-carboxylic acid [1-(2-phenyl-1(r)-{2-[4-(thiophen-2-yl-acetyl)-piperazin-1-yl]-ethylcarbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide
https://huagongshe.com/reaction/917303
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Dimethylformamide | HCID 6228 | — |
| 반응물 | N-(Benzyloxycarbonyl)-D-phenylalanine | HCID 675678 | — |
| 반응물 | Tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate | HCID 735736 | — |
| 반응물 | 2-Benzo[b]thiophen-2-yl-3-oxa-1-azaspiro[4.4]-non-1-en-4-one | HCID 17979617 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 생성물 | Benzo[b]thiophene-2-carboxylic acid [1-(2-phenyl-1(r)-{2-[4-(thiophen-2-yl-acetyl)-piperazin-1-yl]-ethylcarbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide | HCID 10233505 | — |
반응 단계
Analogously to Example 95) 4-[2-2(R)-amino-3-phenyl-propionylamino)-ethyl]-piperazine-1-carboxylic acid tert-butyl ester (obtained starting from Z-D-phenylalanine and N-Boc-4-hydroxyethylpiperazine by reactions and couplings widely described in literature and in part already reported in previous examples) (100 mg, 0.26 mmol) and 2-benzo[b]thiophen-2-yl-3-oxa-1-azaspiro[4.4]-non-1-en-4-one (72 mg, 0.26 mmol) are caused to react in DMF to yield a product which is deprotected and subsequently acylated with thiophen-2-yl-acethyl chloride in CH2Cl2 (as described in Example 94 and purified by flash chromatography using AcOEt as the eluent. 69 mg (0.10 mmol) of benzo[b]thiophene-2-carboxylic acid [1-(2-phenyl-1(R)-{2-[4-(thiophen-2-yl-acetyl)-piperazin-1-yl]-ethylcarbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide are so obtained.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US07273856B2 |
|---|
| 출처 데이터셋 | uspto-grants-2007_09 |
|---|
| ORD ID | ord-c3137d8dd92b41baa88d8d5c6c393f40 |
|---|
| 출처 메모 | uspto-grants-2007_09 |
|---|