HuagongsheHuagongshe Chemistry Print Report · For research reference only
HCID 16228062, compound → HCID 86624171, compound
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | HCID 16228062 | HCID 16228062 | — |
| Reactant | 7-Chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethylsulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine | HCID 57447747 | — |
| Solvent | Toluene | HCID 1140 | — |
| Product | HCID 86624171 | HCID 86624171 | 64% |
Reaction Steps
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 (500 mg, 1.18 mmol) with 4-[(N-methyl-iso-propylamino)-methyl]-benzylamine (270 mg, 1.41 mmol) in toluene (10 mL). Purify by chromatography on silica gel (75 g) eluting with a gradient of 100% DCM to 9:1 DCM/(chloroform:methanol:concentrated NH4OH 80:18:2) to obtain 7-chloro-6-{4-[(N-methyl-iso-propylamino)-methyl]-benzylamino}-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (350 mg, 64%). MS (APCI) m/z: 468 (M+H)+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08680091B2 |
| Source dataset | uspto-grants-2014_03 |
| ORD ID | ord-961fb99baa784d1bb027129aa8b2272f |
| Source note | uspto-grants-2014_03 |