Design and Synthesis of Potential Macrocyclic Zinc Metalloprotease Inhibitors  

作　　者：赵宝祥 SCHAUDT,Marco BLECHERT,Siegfried 

机构地区：[1]Institute of Organic Chemistry School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China [2]Institutfiir Chemie, Technische Universitat Berlin, Strasse des 17. Juni 135, D-10623 Berlin, Germany

出　　处：《Chinese Journal of Chemistry》2006年第8期1080-1085,共6页中国化学（英文版）

摘　　要：A series of succinate-derived macrocyclic amides 1 were synthezized using ring-closing metathesis in the key step. The substrate scope includes rings of 11 to 14 members. The cyclic dicarboxylic acids 1 represent a family of new model compounds for potential zinc metalloprotease inhibitors. The metathesis precursors were provided by amide coupling of tert-butyl 3-carboxyhex-5-enoate 2 with numerous side chain alkenylated amino acid esters of general type 3 derived from L-tyrosine and L-cysteine.A series of succinate-derived macrocyclic amides 1 were synthezized using ring-closing metathesis in the key step. The substrate scope includes rings of 11 to 14 members. The cyclic dicarboxylic acids 1 represent a family of new model compounds for potential zinc metalloprotease inhibitors. The metathesis precursors were provided by amide coupling of tert-butyl 3-carboxyhex-5-enoate 2 with numerous side chain alkenylated amino acid esters of general type 3 derived from L-tyrosine and L-cysteine.

关 键 词：METATHESIS MACROCYCLE aminoacid derivative 

分 类 号：Q556.9[生物学—生物化学]