Synthesis and antitumor activity of a new 7-azaindole derivative

Design and synthesis of Meldrum's acid based 7-azaindole anchored 1,2,3-triazole hybrids as anticancer agents

“…5,6 7-Azaindole is a bioisostere of indole or purine systems, which possesses an electron deficient pyridine ring and a [4,3]-bicyclic indene skeleton with a fused electron-rich pyrrole ring. 7,8 Several marketed drugs contain 7-azaindole (Fig. 1) as the integral part of their structure viz.…”

Phase-Transfer-Catalyzed Asymmetric Annulations of Alkyl Dihalides with Oxindoles: Unified Access to Chiral Spirocarbocyclic Oxindoles

“…8c We therefore applied the developed (4+1) process to the synthesis of compound 18, a key segment of ubrogepant, which was previously prepared by Merck scientists in 11 steps from 15 and 16 via a phase-transfer-catalyzed asymmetric intramolecular alkylation. 14 In contrast, by employing our protocol, this core structure could be efficiently prepared in two steps from more simple pyridine 19 15 and N-Boc 7-azaoxindole 20 16 (Scheme 4B). In brief, we first conducted the (4+1) annulation of 19 and 20 under the standard conditions, which gave spirooxindole 21 in 89% ee at 0.2 mmol scale.…”