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The guide for reaction conditions for obtaining the desired regioisomer of 3,4-dihydroquinoxaline-2(1H)one 16 (SYN) or 17 (ANTI) with the best selectivity.
| Starting pyruvate 12 with additive/ substituted diamine 11 | Ester 12a Acid 12b p-TsOH |
Acid 12b HOBt/DIC |
| 11a–c (EDG or halogen) | 17 (ANTI) (72–91%) | 16 (SYN) (77–86%) |
| 11d–f (EWG) | 16 (SYN) (88–95%) | 17 (ANTI) (93–97%) |
