반응 #42649

ord-df96e00f5e93401da2e695082925d9be

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타was used for the synthesis of 3

실험 절차

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.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07732436B2uspto-grants-2010_06