Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Azetidine | HCID 10422 | — |
| Reactant | (2S)-1-[(6-Chloro-3-pyridinyl)carbonyl]-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine | HCID 59161366 | — |
| Solvent | Isopropanol | HCID 3776 | — |
| Product | HCID 67028737 | HCID 67028737 | 83.6% |
Reaction Steps
(2S)-1-[(6-Chloro-3-pyridinyl)carbonyl]-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Example 26) (69 mg, 0.154 mmol) was transferred into a microwave vial as a solution in isopropanol (1.5 ml). Azetidine (0.208 ml, 3.08 mmol) was added and the clear solution was heated in the microwave to 120° C. for 12 h with stirring. LCMS analysis showed complete conversion. The reaction mixture was concentrated to give the crude material as a colourless gum (206 mg). This was purified by MDAP (High pH system) to give the free base of the title compound as a colourless gum (65 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08536183B2 |
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| Source dataset | uspto-grants-2013_09 |
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| ORD ID | ord-61a91b39c8064fff9ca52bbee2c5bc7c |
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| Source note | uspto-grants-2013_09 |
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