Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Azetidine | HCID 10422 | — |
| Reactant | 4-({(3S)-4-[(6-Chloro-2-methyl-3-pyridinyl)carbonyl]-3-methyl-1-piperazinyl}sulfonyl)-3-methylbenzonitrile | HCID 59161392 | — |
| Solvent | Isopropanol | HCID 3776 | — |
| Product | HCID 67028622 | HCID 67028622 | 43.5% |
Reaction Steps
4-({(3S)-4-[(6-Chloro-2-methyl-3-pyridinyl)carbonyl]-3-methyl-1-piperazinyl}sulfonyl)-3-methylbenzonitrile (may be prepared as described in Example 25) (65 mg, 0.15 mmol) was weighed into a microwave vial and suspended in isopropanol (1.5 ml). Azetidine (0.203 ml, 3.01 mmol) was added and the mixture was heated in the microwave to 120° C. for 18 h with stirring. LCMS analysis showed >80% conversion. The reaction mixture was concentrated to give the crude material as a colourless gum (273 mg). This was purified by MDAP to give the free base of the title compound as a colourless gum (32 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08288388B2 |
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| Source dataset | uspto-grants-2012_10 |
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| ORD ID | ord-22e7d64208c54f38bcc59b44fcc09728 |
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| Source note | uspto-grants-2012_10 |
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