HuagongsheHuagongshe Chemistry Print Report · For research reference only
Hydrochloric Acid → (1S,2S,6R,14R,15S,16R)-5-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-11-ol;hydrochloride
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | Buprenorphine component OF alks-5461 | HCID 9848990 | — |
| Solvent | Acetone | HCID 180 | — |
| Product | (1S,2S,6R,14R,15S,16R)-5-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-11-ol;hydrochloride | HCID 9848989 | — |
Reaction Steps
Conc. HCl (2.6 L) was added to the filtered solution of buprenorphine base (9.65 Kg) in acetone (68 L) at below 15° C. to get pH below 2.0 and stirred for 1.0-2.0 hrs. The HCl salt firmed was filtered, washed with acetone and finally leached with filtered DM water (28 L) at 80° C. and dried. Yield=8.42 Kg.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08710226B2 |
| Source dataset | uspto-grants-2014_04 |
| ORD ID | ord-adb4fd7edfc2437e95d0dd6f521775e8 |
| Source note | uspto-grants-2014_04 |