反応 #42649
ord-df96e00f5e93401da2e695082925d9be
反応条件
詳細条件
See reaction.notes.procedure_details.
後処理
- 1その他was used for the synthesis of 3
実験手順
Starting with the commercially available 2-indolecarboxylic acid, condensation with the ethyl ester of β-alanine in the presence of EDCI and DMAP, provided the indole 4. Methylation of the indole nitrogen with MeI and K2CO3 proceeded in near quantitative yields, rendering the N-methyl indole, which was used for the synthesis of 3. Hydrolysis of esters 4 and 5 followed by the P2O5/MeSO3H mediated cyclization provided the key intermediate aldisine derivatives 8 and 9.