An efficient and convenient method for synthesizing new derivatives of pyrido[2,3-e]pyrrolo[1,2-a][1,4]diazepine-5,10-dione via Sonogashira, Suzuki-Miyaura, and Stille cross-coupling reactions

作者：El Bouakher Abderrahman; Prie Gildas; Aadil Mina; Lazar Said; El Hakmaoui Ahmed; Akssira Mohamed^*; Viaud Massuard Marie Claude

来源：Tetrahedron Letters, 2012, 53(47): 6401-6405.

DOI：10.1016/j.tetlet.2012.09.041

• 2-Aminonicotinic acid
• (S)-3-Bromo-7,8,9,9a-tetrahydro-5H-pyrido[2,3e]pyrrolo[1,2a][1,4]diazepi ne-5,10(11H)-dione
• C-C Cross-coupling reactions

An efficient method for synthesizing new pyrido[2,3-e]pyrrolo[1,2-a][1,4]diazepine-5,10-dione derivatives starting from L-proline methyl ester and 2-aminonicotinic acid is presented. This method employs Pd-catalyzed cross-coupling reaction on the corresponding brominated compound 4 (key intermediate). Sonogashira, Stille, and Suzuki-Miyaura cross-coupling reactions are used to generate products 5a-g, 6, 7a-c, and 8a-e, in good to excellent yields.

• 出版日期2012-11-21