Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | 4-Hydrazinobenzoic acid | HCID 12089 | — |
| Reactant | 2-(2-Hydroxyphenyl)-4H-1,3-benzoxazin-4-one | HCID 135685723 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | Deferasirox | HCID 214348 | 79% |
Reaction Steps
A mixture of methanol (450.0 ml), 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one (30.0 gm) were stir for 10 min at 25-30° C. To the above contents 4-hydrazino benzoic acid (20.03 gm) was added. The contents were heated to reflux temperature 65-70° C. The contents were maintained for 4 hours at 65-70° C. The reaction mass was cooled Slowly to 0-5° C. and maintained it for 1 hour at 0-5° C. The reaction mass was filtered and washed with methanol (30.0 ml). Compound was taken into methylene chloride and stir for 10 min 25-30° C. The contents were heated to reflux temperature (40-45° C.) and maintained the contents for 1 hr at reflux temperature. Cool the contents to 25-30° C. and stirred for 1 hr at 25-30° C. The reaction mass was filtered and washed with methylene chloride (30.0 ml). Dried the compound at 60-65° C. Yield: 79.0%.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08907083B2 |
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| Source dataset | uspto-grants-2014_12 |
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| ORD ID | ord-d759662232c248b58df24119fecbdd49 |
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| Source note | uspto-grants-2014_12 |
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