Synthesis of 5-(3-Tert-Butylamino-2-Hydroxy) Propoxy-3,4-Dihydrocarbostyril

5-(3-tert-Butylamino-2-hydroxy) propoxy-3, 4-dihydrocarbostyril ( 1 , carteolol) was prepared by an acid-catalyzed cyclization of the N-pivaloylamino-ester ( 5 ), which was obtained by using organolithiation of m-pivaloylanisidine, followed by Wittig and catalytic hydrogenation reactions. The total yield of 1 obtained from m-anisidine ( 2 ) is 21%.