HuagongsheHuagongshe Chemistry Print Report · For research reference only
Carbonate Ion → Arbaclofen Placarbil
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Carbonate Ion | HCID 19660 | — |
| Reactant | Arbaclofen | HCID 44602 | — |
| Reactant | {[(1S)-isobutanoyloxyisobutoxy]carbonyloxy} succinimide | HCID 68997310 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | tert-Butyl methyl ether | HCID 15413 | — |
| Product | Arbaclofen Placarbil | HCID 11281011 | — |
Reaction Steps
A 20-L pilot plant equipped with a mechanical stirrer and a nitrogen inlet was charged with NHS-carbonate, 1-S-[[[(isobutyryloxy)isobutyroxy]carbonyl]oxy]-2,5-pyrrolidinedione (20b), 1.31 kg, 4.7 mol) and (R)-baclofen (431 g; overall 1.2 eq. of R-baclofen) in a mixture of methyl tert-butyl ether (MTBE) and water (3:1; 10 L). The resulting suspension is stirred for 24 hours at room temperature.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08062870B2 |
| Source dataset | uspto-grants-2011_11 |
| ORD ID | ord-b362f98e6fa6415ca804467edc06d6ae |
| Source note | uspto-grants-2011_11 |