Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sodium Carbonate | HCID 10340 | — |
| Reactant | Lithium Chloride | HCID 433294 | — |
| Reactant | (Triethylsilyl)acetylene | HCID 637947 | — |
| Reactant | 2-Amino-5-chloro-3-iodopyridine | HCID 11076010 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | HCID 57774343 | HCID 57774343 | 44% |
Reaction Steps
A mixture of 40 (9.5 g, 37.3 mmol) was dissolved in 320 mL of DMF and triethylsilylacetylene (20 mL, 112 mmol), Pd2Cl2 (dppf)2 (1.52 g, 1.9 mmol), lithium chloride (1.58 g, 37.3 mmol) and 2M Na2CO3 (7.9 mL, 74.7 mL) were added and the mixture was stirred and refluxed at 90° C. for 15 h under nitrogen. Diluted with ethyl acetate-ether mixture (1:1) and the organic phase washed with water and brine then dried (Na2SO4) and concentrated in vacuo. The residue was subjected to flash chromatography (20% EtOAc/80% hexanes) to give 4.37 g (44%) of the desired product 41. 1H NMR (500 MHz, CDCl3) 9.4 (bs, 1H), 8.2 (s, 1H), 7.9 (s, 1H), 6.6 (s, 1H), 0.9 (t, 9H), 0.75 (q, 6H).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08722889B2 |
|---|
| Source dataset | uspto-grants-2014_05 |
|---|
| ORD ID | ord-0bf79abcb7534ae896a7308674954e68 |
|---|
| Source note | uspto-grants-2014_05 |
|---|