Table 3.
4a 89% yield, 90% eeb |
4b 96% yield, 92% ee |
4c 99% yield, 86% ee |
4d 86% yield, 88% ee |
4e 92% yield, 89% ee |
4f 88% yield, 90% ee |
4g 81% yield, 83% ee |
4h 99% yield, 81% eeb |
4i 91% yield, 93% ee |
4j 57% yield, 73% eeb |
4k 60% yield, 73% eeb |
4l, R = H: NR 4m, R = Ph: NR |
All reactions were performed with 1.0 equiv of indole nucleophile and 1.1 equiv of 1 at ambient temperature. Isolated yield. % ee was determined by chiral HPLC.
1.1 equiv of Cs2CO3 was added.