Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
[4-(Morpholin-4-ylmethyl)phenyl]methanamine → 7-chloro-6-[4-(morpholin-4-ylmethyl)-benzylamino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | [4-(Morpholin-4-ylmethyl)phenyl]methanamine | HCID 2795501 | — |
| 반응물 | 7-Chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethylsulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine | HCID 57447747 | — |
| 생성물 | 7-chloro-6-[4-(morpholin-4-ylmethyl)-benzylamino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine | HCID 86624168 | 67.1% |
반응 단계
Use a method similar to the General Procedure 1-2 to couple 7-chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethanesulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine (400 mg, 0.94 mmol) with 4-(morpholin-4-ylmethyl)-benzylamine (291 mg, 1.41 mmol). Purify by chromatography on silica gel (80 g, pre-packed cartridge) eluting with hexane/EtOAc (1:0 to 2:1 gradient) to obtain 7-chloro-6-[4-(morpholin-4-ylmethyl)-benzylamino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (304 mg, 67%). MS (APCI+) m/z: 482 (M+H)÷.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08680091B2 |
| 출처 데이터셋 | uspto-grants-2014_03 |
| ORD ID | ord-607175374a924bafa502e4877339fda0 |
| 출처 메모 | uspto-grants-2014_03 |