Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Pyridine | HCID 1049 | — |
| Reactant | P,P-Diphenylphosphinic azide | HCID 199401 | — |
| Reactant | 2-Amino-6-(piperidin-1-ylmethyl)pyridine | HCID 18771671 | — |
| Reactant | 5-(4-Carboxy-thiazol-2-yl)-indole-1-carboxylic acid tert-butyl ester | HCID 69411139 | — |
| Solvent | Toluene | HCID 1140 | — |
| Product | HCID 59110594 | HCID 59110594 | — |
Reaction Steps
To a solution of 5-(4-carboxy-thiazol-2-yl)-indole-1-carboxylic acid tert-butyl ester (2.65 g, 7.69 mmol), molecular sieves, and 100 mL of dry toluene was added TEA (1.6 mL, 11.5 mmol). The resulting solution was stirred for 20 min then DPPA (2.5 mL, 11.6 mmol) was added and the resulting solution was stirred at 80° C. for 40 min. 6-Piperdin-1-ylmethyl-pyridin-2-ylamine (1.64 g, 8.6 mmol) and pyridine (1.0 mL, 12.4 mmol) were added and the mixture was stirred at 80° C. for another 14 h. The molecular sieves were filtered off and washed with CH2Cl2 and MeOH. The filtrate was concentrated in vacuo and the resulting residue was purified by flash chromatography on silica gel using 3% MeOH/CH2Cl2 to give a brown solid. MS m/z: 533 (M+1). Calc'd for C28H32N6O3S-532.66.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07196104B2 |
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| Source dataset | uspto-grants-2007_03 |
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| ORD ID | ord-9172118bbfb649bd989c575ddf60c8e8 |
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| Source note | uspto-grants-2007_03 |
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