Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Carbamate | HCID 276 | — |
| Reactant | Pyridine | HCID 1049 | — |
| Reactant | 4-Nitrophenyl chloroformate | HCID 82129 | — |
| Reactant | HCID 437068 | HCID 437068 | — |
| Reactant | Methyl 6-aminopyridazine-3-carboxylate | HCID 14536428 | — |
| Reactant | 2,3-Dihydro-1H-pyrrolo[3,4-c]pyridine--hydrogen chloride (1/2) | HCID 18953644 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 68752163 | HCID 68752163 | — |
Reaction Steps
Methyl 6-aminopyridazine-3-carboxylate (2 g, 13.06 mmol) was suspended in dichloromethane (50 ml) followed by addition of dry pyridine (1.265 ml, 15.67 mmol) under nitrogen. To this suspension was added a dichloromethane solution of 4-nitrophenyl carbonochloridate (2.99 g, 14.37 mmol) via syringe at ambient temperature. The mixture was stirred overnight to give a suspension that was concentrated to half volume under a stream of nitrogen. 2,3-Dihydro-1H-pyrrolo[3,4-c]pyridine, dihydrochloride (2.52 g, 13.06 mmol) was dissolved in 30 ml dimethylformamide with triisopropylethylamine (6.84 ml, 39.2 mmol) and added to the carbamate mixture via syringe. After stirring the mixture overnight and removing most of the solvent under vacuum, water was added; and the resulting suspension was stirred for 30 minutes and filtered to give a solid which was washed with water. Flash chromatography of the dried solid gave the title compound.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US09302989B2 |
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| Source dataset | uspto-grants-2016_04 |
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| ORD ID | ord-ebb8fbd01e77457496f72ccdaebf6325 |
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| Source note | uspto-grants-2016_04 |
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