HuagongsheHuagongshe Chemistry Print Report · For research reference only
1-Propanesulfonic acid → 3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}-phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester propanesulfonate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1-Propanesulfonic acid | HCID 78938 | — |
| Reactant | 3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester | HCID 67471184 | — |
| Solvent | Ethyl Acetate | HCID 8857 | — |
| Product | 3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}-phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester propanesulfonate | HCID 86677406 | — |
Reaction Steps
At room temperature, 3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester (Example 6f, 100 mg) was dissolved in ethyl acetate (10 mL), a solution of 1-propanesulfonic acid [CAS No. 5284-66-2] (13.5 mg) in ethyl acetate (1 mL) was added dropwise thereto. The resulting mixture was stirred at room temperature for 22 hours, and the precipitated solid was filtered. The solids recovered by filtration were washed with ethyl acetate and TBME, and dried. The captioned compound (90 mg) was obtained.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08436009B2 |
| Source dataset | uspto-grants-2013_05 |
| ORD ID | ord-2e44d4a1045040d58a204d93b19e7e9b |
| Source note | uspto-grants-2013_05 |