HuagongsheHuagongshe Chemistry Print Report · For research reference only
Hydrochloric Acid → (R)-ethyl 4-(4-(amino(4'-chlorobiphenyl-2-yl)methyl)piperidin-1-yl)benzoate hydrochloride salt
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | ethyl 4-(4-((R)-(4'-chlorobiphenyl-2-yl)((S)-1,1-dimethylethylsulfinamido)methyl)piperidin-1-yl)benzoate | HCID 58080205 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | (R)-ethyl 4-(4-(amino(4'-chlorobiphenyl-2-yl)methyl)piperidin-1-yl)benzoate hydrochloride salt | HCID 86661881 | 215% |
Reaction Steps
HCl (1.16 ml, 4.63 mmol, 4.0M in dioxane) was added to a solution of ethyl 4-(4-((R)-(4′-chlorobiphenyl-2-yl)((S)-1,1-dimethylethylsulfinamido)methyl)piperidin-1-yl)benzoate (INTERMEDIATE 128, 0.128 g, 0.23 mmol) in MeOH (3.5 ml) and the reaction mixture was stirred at r.t. for 3 hours. The reaction mixture was concentrated under reduced pressure and dried under vacuum to provide (R)-ethyl 4-(4-(amino(4′-chlorobiphenyl-2-yl)methyl)piperidin-1-yl)benzoate hydrochloride salt (INTERMEDIATE 133, STEP 1, 0.12 g), which was used in the preparation of INTERMEDIATE 133, STEP 2 without further purification.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09018381B2 |
| Source dataset | uspto-grants-2015_04 |
| ORD ID | ord-7dbca12e0ddc483693fb97cfa8e576e2 |
| Source note | uspto-grants-2015_04 |