Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Bromobenzene | HCID 7961 | — |
| Reactant | Tetrabutylammonium Fluoride | HCID 2724141 | — |
| Reactant | 5-Ethynyl-2,8-dimethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole | HCID 59455000 | — |
| Solvent | Water | HCID 962 | — |
| Product | HCID 59322146 | HCID 59322146 | 4.4% |
Reaction Steps
A mixture of 5-ethynyl-2,8-dimethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (171 mg, 0.76 mmol), bromo benzene (100 mg, 0.6 mmol), dichlorobistriphenylphosphine palladium(II) (12 mg, 0.018 mmol) and TBAF.3H2O (567 mg, 1.8 mmol) were heated 80° C. for 5 min by microwave. After completion of reaction (monitored by TLC), the mixture was poured into water (10 mL) and extracted with EtOAc (2×20 mL). The organic layer was dried over sodium sulfate and concentrated under vacuum and the crude product purified by column chromatography using silica gel (100-200 mesh) and 1% MeOH in DCM as eluent, followed by reverse phase chromatography to obtain 8 mg of 2,8-dimethyl-5-phenylethynyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole. 1H NMR (CDCl3, freebase) δ (ppm): 7.55 (d, 2H), 7.50 (d, 1H), 7.40-7.31 (m, 3H), 7.20 (s, 1H), 7.10 (d, 1H), 3.70 (s, 2H), 3.0 (t, 2H), 2.90 (t, 2H), 2.60 (s, 3H), 2.45 (s, 3H).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08907097B2 |
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| Source dataset | uspto-grants-2014_12 |
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| ORD ID | ord-4cc3424123de46f7817a88878a3f76d1 |
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| Source note | uspto-grants-2014_12 |
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