Efficient solution phase synthesis of 2-(N-acyl)-aminobenzimidazoles

PP Seth, DE Robinson, EA Jefferson, EE Swayze

Index: Seth, Punit P.; Robinson, Dale E.; Jefferson, Elizabeth A.; Swayze, Eric E. Tetrahedron Letters, 2002 , vol. 43, # 41 p. 7303 - 7306

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Citation Number: 25

Abstract

An efficient solution phase protocol for the synthesis of 2-(N-acyl)-aminobenzimidazoles is reported. The 2-(N-acyl)-aminobenzimidazole ring system was assembled using SNAr reactions, nitro group reduction, acylthiourea formation and cyclization with EDC. The acyl protected 2-aminobenzimidazole derivatives were obtained in high yield and purity without purification of intermediates or final products. This reaction sequence eliminates the use of ...