Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | Methanesulfonyl chloride | HCID 31297 | — |
| Reactant | HCID 89443903 | HCID 89443903 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 71533617 | HCID 71533617 | 65.1% |
Reaction Steps
To a mixture of 3-(4-Fluoro-phenyl)-1-[1-(4-fluoro-phenyl)-ethyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine (enantiomer 1) (7e) (0.120 g, 0.353 mmol) and triethylamine (0.135 ml, 1.06 mmol) in CH2Cl2 at 0° C. was added methanesulfonyl chloride (49 mg, 0.424 mmol) and the mixture was stirred at 25° C. for 16 h. The crude product was purified by reverse phase HPLC (CH3CN/water gradient with 0.1% trifluoroacetic acid) to give 96 mg of 3-(4-Fluoro-phenyl)-1-[(R)-1-(4-fluoro-phenyl)-ethyl]-5-methanesulfonyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine (9a).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US09127001B2 |
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| Source dataset | uspto-grants-2015_09 |
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| ORD ID | ord-11f38a8727294f0b827c254f6a317f06 |
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| Source note | uspto-grants-2015_09 |
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