HuagongsheHuagongshe Chemistry Print Report · For research reference only
Hydrochloric Acid → Erlotinib Hydrochloride
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | Ethyl formate | HCID 8025 | — |
| Reactant | Erlotinib | HCID 176870 | — |
| Solvent | Isopropanol | HCID 3776 | — |
| Product | Erlotinib Hydrochloride | HCID 176871 | 93.6% |
Reaction Conditions
| Temperature | 5 °C |
|---|
Reaction Steps
10.0 g crystal form IV of erlotinib base was added to 200 ml ethyl formate, heated to 0-10° C., 6.4 g isopropanol saturated with HCl gas was added dropwise, after dripping, stirred for 30 minutes while maintaining the temperature, stirred for 1 hour at 0-15° C. before filtration, dried at 50° C. to obtain 10.2 g sample of crystal form A. The yield was 93.6% and the purity was 99.7% (by HPLC).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08653264B2 |
| Source dataset | uspto-grants-2014_02 |
| ORD ID | ord-aecce3c5959c49b5b418011801015501 |
| Source note | uspto-grants-2014_02 |