| abstract |
The invention relates to the field of macrolides. It concerns 12-(2'-cyclopentylvinyl)-11,28-dioxa-4-azatricyclo[22.3.1.0 4,9 ]octacos-18-ene or -14,18-diene and 11-(2′-cyclopentylvinyl)-10,27-dioxa-4-azatricyclo[21.3.1.0 4,8 ]heptacos-17-ene or -13,17-diene derivatives, in particular the compounds of formula In wherein the substituents have various significances. They are prepared by a process comprising ring contraction accompanied by appropriate derivatization. They possess interesting pharmacological activity as immunosuppressant and antiproliferative, antiinflammatory, and chemotherapeutic drug resistance reversing agents. |