Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | HCID 86670536 | HCID 86670536 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | HCID 86670535 | HCID 86670535 | 103.2% |
Reaction Steps
A 100 mL vial equipped with stir bar was charged with tert-butyl 5′-(5-(3,5-bis(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3′-oxospiro[azetidine-3,1′-isoindoline]-1-carboxylate (Preparation 21, 240 mg, 0.4 mmol) and anhydrous methanol (25 mL). A methanolic solution of HCl (1 mL of a 1.25M solution) was added and the reaction was heated to 65° C. for 6 hours. The reaction was cooled and concentrated under vacuum. The residue was rinsed with diethyl ether, concentrated under vacuum, and subsequently placed under high vacuum for 1 hour to afford the intermediate (216 mg, 95%) as an HCl salt. m/z (CI) 524 [M+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08466115B2 |
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| Source dataset | uspto-grants-2013_06 |
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| ORD ID | ord-9a005ddd422647039b0b7033ad8f8e65 |
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| Source note | uspto-grants-2013_06 |
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