TY - JOUR AU - Guedes de la Cruz, Gema; Svobodova, Barbora; Lichtenegger, Michaela; Tiapko, Oleksandra; Groschner, Klaus; Glasnov, Toma TI - Intensified Microwave-Assisted N-Acylation Procedure – Synthesis and Activity Evaluation of TRPC3 Channel Agonists with a 1,3-Dihydro-2H-benzo[d]imidazol-2-one Core SN - 0936-5214 SN - 1437-2096 PY - 2017 JO - Synlett JF - Synlett LA - EN VL - 28 IS - 06 SP - 695 EP - 700 ET - 2016/12/08 DA - 2017/03/16 KW - microwave synthesis KW - acylation KW - amides KW - Ca2+-signaling KW - TRPC ion channels KW - agonist AB - Upon controlled microwave heating and using cyanuric chloride as a coupling reagent, an efficient amidation procedure for the synthesis of 1,3-dihydro-2H-benzo[d]imidazol-2-one-based agonists of TRPC3/6 ion channels has been developed. Compared to the few conventional protocols, a drastic reduction in processing time from ca. 2 days down to 10 minutes was achieved accompanied by significantly improved product yields. The robustness of the method was confirmed by 18 additional examples including aromatic, aliphatic, and heterocyclic amines and acids. The obtained agonists were screened for biological activity at 1 μM concentration and few structure–activity relations have been established. PB - © Georg Thieme Verlag DO - 10.1055/s-0036-1589472 UR - http://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0036-1589472 ER -