Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sodium hydride | HCID 24758 | — |
| Reactant | Dimethylthiocarbamoyl chloride | HCID 27871 | — |
| Reactant | 2-[4-(4-Hydroxyphenyl)butyl]-1H-isoindole-1,3(2H)-dione | HCID 22054451 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | HCID 58912942 | HCID 58912942 | 59.4% |
Reaction Steps
A suspension of sodium hydride (60% in mineral oil, 0.44 g, 0.11 mmol) in anhydrous DMF (10 mL) was cooled to 0° C. and added to a solution of 2-[4-(4-hydroxyphenyl)-butyl]isoindole-1,3-dione 8 (2.95 g, 10 mmol) in DMF (15 mL). The mixture was stirred at 0° C. for 30 min and then at room temperature for an additional one hour. A solution of dimethylthiocarbamic acid chloride (1.35 g, 11 mmol) in DMF (10 mL) was then added. The reaction mixture was stirred at room temperature first for 16 h and then at 50° C. for 1 h, cooled back to room temperature and quenched with methanol (10 mL). The mixture was concentrated under vacuum and the residue was purified by flash silica gel column chromatography eluting with CH2Cl2/hexanes/EtOAc (10:1:0.2, v/v) to give the desired product 9 as a yellowish solid (2.27 g, 59% yield). 1H NMR (300 MHz, CDCl3) δ 1.72 (m, 4H), 2.67 (m, 2H), 3.33 (s, 3H), 3.45 (s, 3H), 3.71 (m, 2H), 6.95 (d, 2H), 7.18 (d, 2H), 7.70 (m, 2H), 7.84 (m, 2H). m/z (ESI): 383 [C21H22N2O3S+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07368451B2 |
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| Source dataset | uspto-grants-2008_05 |
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| ORD ID | ord-f71a7d1137ec4cc4854b946151391cbf |
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| Source note | uspto-grants-2008_05 |
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