A Novel synthesis of 5,6‐dihydro‐2,3‐bisaryl‐8H‐imidazo[2,1‐c][1,4]thiazine

Abstract

Bisaryl‐8H‐imidazo[2,1‐c][1,4]thiazines were prepared from the corresponding 2‐thiomethylimidazoles. A novel and efficient synthesis is presented for these intermediates based on the condensation of benzils with protected 2‐thioacetaldehydes.

Synthesis of Boronocysteine

“…Bromoacetaldehyde dimethyl acetal 3a was converted into the corresponding sulfide 3b by reaction with p-methoxybenzyl thiol (PMBSH) and sodium hydroxide (Scheme 3). 13 After deprotection of the acetal, the aldehyde 4 14 was then converted into sulfinimine 5 through condensation with the sulfinimide. 16 With the required sulfinimide in hand, the Cu-catalysed borylation reaction was investigated.…”