ChemInform Abstract: Potent Anticonflict Activity and Lessening of Memory Impairment with a Series of Novel (1)Benzothieno(2,3‐c)pyridines and 1,2,3,4‐Tetrahydro‐( 1)benzothieno(2,3‐c)pyridines.

Abstract

Novel (1)Benzothieno(2,3-c)pyridines and 1,2,3,4-Tetrahydro-( 1)benzothieno(2,3-c)pyridines. -The benzothienopyridines (IV) are prepared by esterification of the amino acid (I) followed by cyclization reaction with formaldehyde (III) . N-Protection of (IVb) and subsequent deesterification yield the carboxylic acid (VI) which is successively coupled with cyclohexylamine (VII) and deprotected to give the amide (VIII). The amides (X) are formed by reaction of (IVb) with the acyl chlorides (IX) . Oxidation of (IVb) followed by deesterification yields the carboxylic acid (XI) which is coupled with amines such as (XII) to produce the corresponding amides (XIII). Among the compounds prepared, the derivatives (IVb), (VIII), and (XIIIa) show the best anticonflict and antiscopolamine amnesia-reversal activity. -(KAWAKUBO, H.; OKAZAKI, K.; NAGATANI, T.; TAKAO, K.; HASIMOTO, S.; SUGIHARA, T.; J.