选择性酰化氨基,对羟基而言.pdfVIP

J. Chil. Chem. Soc., 56, Nº 4 (2011) HIGHLY EFFICIENT AND VERSATILE ACETYLATION OF ALCOHOLS, PHENOLS AND AMINES CATALYZED BY METHYLENEDIPHOSPHONIC ACID (MDP) UNDER SOLVENT-FREE CONDITIONS MINHAO XIE*, HONGYONG WANG, JUN WU, YONGJUN HE, YALING LIU, PEI ZOU *Jiangsu Institute of Nuclear Medicine, Wuxi, 214063, P. R. China (Received: March 1, 2011 - Accepted: July 12, 2011) ABSTRACT Methylenediphosphonic Acid (MDP) was found to be a simple, cheap and reusable heterogeneous catalyst for the acetylation of structurally diverse alcohols, phenols and amines with acetic anhydride under solvent-free conditions at room temperature. This method showed preferential selectivity for the acetylation of the amino group in the presence of hydroxyl group. The method is very mild and the yields were in excellent. Keywords: Bisphosphonic acid, MDP, Solvent-free, Acetylation. INTRODUCTION With increasing environmental concerns and the regulatory constraints faced in the synthesis of valuable industrial and pharmaceutical compounds, the development of new synthetic methods and reactions using new and environmental friendly reagents is becoming more attractive. The acetylation of alcohols is an important and E-mail: xiemh0704@ Fax number: +086 510 frequently used transformation in organic synthesis 1. The most commonly used reagent combination for this reaction uses an acid anhydride in the presence of an acid or base catalyst 2 . The various Scheme 1: Acetylation of Alcohols and Phenols catalysts developed for acetylation