HuagongsheHuagongshe Chemistry Print Report · For research reference only
Hydrochloric Acid → Btk inhibitor 1 (R enantioMer hydrochloride)
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate | HCID 59799012 | — |
| Solvent | Diethyl Ether | HCID 3283 | — |
| Solvent | 1,4-Dioxane | HCID 31275 | — |
| Product | Btk inhibitor 1 (R enantioMer hydrochloride) | HCID 78357770 | 88% |
Reaction Steps
Compound 35 (700 mg, 1.48 mmol, 1 equiv) was dissolved in dioxane (8 mL). A solution of hydrogen chloride in dioxane (4 mL of a 4 N solution in dioxane, 16 mmol, 10.7 equiv) was added and the reaction was stirred at room temperature overnight. The reaction was diluted with diethyl ether (20 mL) and the resulting solids were collected by filtration under a stream of nitrogen. The product was further dried in a vacuum oven to yield 36 (550 mg, 88% yield) as an off-white solid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09422295B2 |
| Source dataset | uspto-grants-2016_08 |
| ORD ID | ord-e9c4b178b3cf4752b19cb579fcae36db |
| Source note | uspto-grants-2016_08 |