Table 1.
Library of isoxazolino-β-ketoamides.
| Entry | Acyl Ketene | Chloro-Oxime | Amine | Product | Yield |
|---|---|---|---|---|---|
| 1 | {1} | {1} | {1} | 5{1,1,1) | 80% |
| 2 | {1} | {1} | {2} | 5{1,1,2) | 79% |
| 3 | {1} | {1} | {3} | 5{1,1,3} | 30% |
| 4 | {1} | {1} | {4} | 5{1,1,4} | 40% |
| 5 | {1} | {1} | {5} | 5{1,1,5} | 40% |
| 6 | {1} | {1} | {6} | 5{1,1,6} | 51% |
| 7 | {1} | {1} | {7} | 5{1,1,7} | 76% |
| 8 | {1} | {1} | {8} | 5{1,1,8} | 88% |
| 9 | {1} | {2} | {1} | 5{1,2,1) | 75% |
| 10 | {1} | {2} | {2} | 5{1,2,2) | 76% |
| 11 | {1} | {2} | {3} | 5{1,2,3} | 31% |
| 12 | {1} | {2} | {4} | 5{1,2,4} | 44% |
| 13 | {1} | {2} | {5} | 5{1,2,5} | 31% |
| 14 | {1} | {2} | {6} | 5{1,2,6} | 50% |
| 15 | {1} | {2} | {7} | 5{1,2,7} | 78% |
| 16 | {1} | {2} | {8} | 5{1,2,8} | 83% |
| 17 | {1} | {3} | {1} | 5{1,3,1) | 81% |
| 18 | {1} | {3} | {2} | 5{1,3,2) | 80% |
| 19 | {1} | {3} | {3} | 5{1,3,3} | 19% |
| 20 | {1} | {3} | {4} | 5{1,3,4} | 48% |
| 21 | {1} | {3} | {5} | 5{1,3,5} | 41% |
| 22 | {1} | {3} | {6} | 5{1,3,6} | 38% |
| 23 | {1} | {3} | {7} | 5{1,3,7} | 75% |
| 24 | {1} | {3} | {8} | 5{1,3,8} | 75% |
| 25 | {2} | {1} | {1} | 5{2,1,1) | 30% |
| 26 | {2} | {1} | {2} | 5{2,1,2) | 50% |
| 27 | {2} | {1} | {3} | 5{2,1,3} | 8% |
| 28 | {2} | {1} | {4} | 5{2,1,4} | 15% |
| 29 | {2} | {1} | {5} | 5{2,1,5} | 35% |
| 30 | {2} | {1} | {6} | 5{2,1,6} | 44% |
| 31 | {2} | {1} | {7} | 5{2,1,7} | 55% |
| 32 | {2} | {1} | {8} | 5{2,1,8} | 64% |
| 33 | {2} | {2} | {1} | 5{2,2,1) | 60% |
| 34 | {2} | {2} | {2} | 5{2,2,2) | 58% |
| 35 | {2} | {2} | {3} | 5{2,2,3} | 17% |
| 36 | {2} | {2} | {4} | 5{2,2,4} | 31% |
| 37 | {2} | {2} | {5} | 5{2,2,5} | 30% |
| 38 | {2} | {2} | {6} | 5{2,2,6} | 33% |
| 39 | {2} | {2} | {7} | 5{2,2,7} | 60% |
| 40 | {2} | {2} | {8} | 5{2,2,8} | 60% |
| 41 | {2} | {3} | {1} | 5{2,3,1) | 62% |
| 42 | {2} | {3} | {2} | 5{2,3,2) | 42% |
| 43 | {2} | {3} | {3} | 5{2,3,3} | 12% |
| 44 | {2} | {3} | {4} | 5{2,3,4} | 46% |
| 45 | {2} | {3} | {5} | 5{2,3,5} | 60% |
| 46 | {2} | {3} | {6} | 5{2,3,6} | 45% |
| 47 | {2} | {3} | {7} | 5{2,3,7} | 70% |
| 48 | {2} | {3} | {8} | 5{2,3,8} | 68% |
| 49 | {3} | {1} | {1} | 5{3,1,1) | 49% |
| 50 | {3} | {1} | {2} | 5{3,1,2) | 78% |
| 51 | {3} | {1} | {3} | 5{3,1,3} | 23 |
| 52 | {3} | {1} | {4} | 5{3,1,4} | 31% |
| 53 | {3} | {1} | {5} | 5{3,1,5} | 37% |
| 54 | {3} | {1} | {6} | 5{3,1,6} | 44% |
| 55 | {3} | {1} | {7} | 5{3,1,7} | 52% |
| 56 | {3} | {1} | {8} | 5{3,1,8} | 62% |
| 57 | {3} | {2} | {1} | 5{3,2,1) | 77% |
| 58 | {3} | {2} | {2} | 5{3,2,2) | 70% |
| 59 | {3} | {2} | {3} | 5{3,2,3} | 18% |
| 60 | {3} | {2} | {4} | 5{3,2,4} | 39% |
| 61 | {3} | {2} | {5} | 5{3,2,5} | 35% |
| 62 | {3} | {2} | {6} | 5{3,2,6} | 43% |
| 63 | {3} | {2} | {7} | 5{3,2,7} | 54% |
| 64 | {3} | {2} | {8} | 5{3,2,8} | 62% |
| 65 | {3} | {3} | {1} | 5{3,3,1) | 76% |
| 66 | {3} | {3} | {2} | 5{3,3,2) | 62% |
| 67 | {3} | {3} | {3} | 5{3,3,3} | 9% |
| 68 | {3} | {3} | {4} | 5{3,3,4} | 34% |
| 69 | {3} | {3} | {5} | 5{3,3,5} | 69% |
| 70 | {3} | {3} | {6} | 5{3,3,6} | 32% |
| 71 | {3} | {3} | {7} | 5{3,3,7} | 63% |
| 72 | {3} | {3} | {8} | 5{3,3,8} | 40% |