PREPARATION OF ALPHA-6-DEOXYTETRACYCLINES

专利名称：PREPARATION OF ALPHA-6-DEOXYTETRACYCLINES

发明人：RENATO BROGGI,GINO COTTI申请号：AU5250273申请日：19730222公开号：AU5250273A公开日：19740822

摘要：1418137 Preparing tetracycline compounds ANKERFARM SpA 19 Feb 1973 [24Feb 1972] 8119/73 Heading C2C Alpha-6-deoxy-tetracyclines of Formula (II) wherein Y ishydrogen, fluorine, chlorine, bromine or iodine, and R is hydrogen, hydroxyl or a group: -O-CO-R1 in which R1 is C 1-6 alkyl are prepared by hydrogenating a 6-demethyl - 6 -deoxy - 6 - methylene - tetracycline of Formula (I): wherein Y and R are as defined above,at a hydrogen pressure of 1 to 150 kg./cm.2 for 1-8 hours at 15‹ to 80‹ C. in a polarsolvent, in the present of, as catalyst, a solution in said solvent of a complex of a ligandwhich is a tertiary organic phosphine, arsine or stibine with a metal which is rhodium,palladium, ruthenium, osmium, iridium, platinum or nickel, said complex containinghalogen bound directly to the metal. Suitable ligands are triphenylphosphine,

tributylphosphine, triethylphosphine, diethylphenylphosphine, diphenylethylphosphine,alkylphosphoric esters, triphenylstibine and triphenylarsine. The preferred metal isrhodium, the catalyst being prepared by reacting rhodium chloride with the ligand in thereaction medium. Polar solvents used are C 1-4 mono- or polyhydric alcohols, N,N1-dimethylformamide, N,N1-dimethylacetamide, dioxan, tetrahydrofuran, methoxyethanol,ethoxyethanol, acetonitrile or pyridine.

申请人：ANKERFARM S.P.A.

更多信息请下载全文后查看