Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo–keto reductase 1C3 target affinity. Issue 8 (9th July 2019)

• Record Type: Journal Article
• Authors: Santos, Ana R. N.; Sheldrake, Helen M.; Ibrahim, Ali I. M.; Danta, Chhanda Charan; Bonanni, Davide; Daga, Martina; Oliaro-Bosso, Simonetta; Boschi, Donatella; Lolli, Marco L.; Pors, Klaus
• Is Part Of: MedChemComm. Volume 10:Issue 8(2019)
• Page Start: 1476
• Page End: 1480
• Publication Date: 2019-07-09
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c9md00201d
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Abstract : Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Here, we report on the use of transition-metal mediated [2 + 2 + 2] cyclotrimerisation of alkynes to generate tricyclic THIQs with potential to selectively inhibit AKR1C3.