HuagongsheHuagongshe Chemistry Print Report · For research reference only
Chloride → 4-[3-(2-Azetidin-1-ylmethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Chloride | HCID 312 | — |
| Reactant | Azetidine | HCID 10422 | — |
| Reactant | Thionyl Chloride | HCID 24386 | — |
| Reactant | HCID 22317746 | HCID 22317746 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | 4-[3-(2-Azetidin-1-ylmethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one | HCID 22317406 | — |
Reaction Steps
The title compound was prepared from 4-[3-(2-hydroxymethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one (Example 286) (255 mg, 0.50 mmol) by reaction with thionylchloride in CH2Cl2 and subsequent treatment of the corresponding crude chloride with azetidine in DMF according to the general procedure of example 288. Obtained as an off-white solid (153 mg, 56%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US06949542B2 |
| Source dataset | uspto-grants-2005_09 |
| ORD ID | ord-3d2dc8db46f14436bf3664bf86a81d50 |
| Source note | uspto-grants-2005_09 |