SHEKHAR, SHASHANK,FRANCZYK, THADDEUS S.,BARNES, DAVID M.,DUNN, TRAVIS B.,HAIGHT, ANTHONY R.,CHAN, VINCENT S.
申请号：
PE0000782013
公开号：
PE10862013A1
申请日:
2011.07.15
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Relating to a method for preparing N - (4 - (Tert Butyl) - 5 - (2 - [- 3.4 - dihydropyrimidine - 1 (2H) - yl) - 2-methoxyphenyl) naftalen - 2 (IL -) metansulfonamida Compound or a Salt thereof, which comprises the compound (sulfonamidar 5) by a transition metal Catalyst Precursor or as N precursor of palladium catalyst and a ligand such as phosphine,In the presence of a base such as Cesium carbonate, Sodium carbonate, among others, and a Solvent such as tetrahydrofuran, n-methyl pyrrolidone, among others, where is perfluorobutilo A1A, phenyl phosphine, among others, and is 7,7,9,9 - Tetramethyl - 8 - (2 , 4, 6 - triisopropilbifenil - 2 - yl) - 1.4 - dioxa Fos - 8 - Faespiro [4,5] Dean, tetrametil.1. 2,2,6,6-tetramethyl-1 - (2 , 4, 6 - triisopropilbifenil - 2 - il) fosfinano, among others.The Compound (5) was prepared by reacting the 1 - (3 - (Tert Butyl - 5 - 6 - hidroxinaftalen - 2 - il) - 4-methoxyphenyl) pyrimidine 2,4 (1H, 3H) - dione (Compound 4) with perfluorobutansulfonilo fluoride in the presence of a base and a solvent.Compound 4 was prepared by coupling 1 - (Tert Butyl 3 - 5 - iodo - 4-methoxyphenyl) pyrimidine 2,4 (1H, 3H) - dione with acid - 2 - 6 - hidroxinaftalen ilboronico in the presence of a phosphine ligand as butilfosfina Tri -, tris (2-furyl) phosphine, among others, a precursor of The Catalyst of transition metal ta L diacetate as PALLADIUM (ii), tetrakis (trifenilfosfin) palladium (0), among others.A base such as Cesium Cesium carbonate, fluoride, among others. These compounds are inhibitors of HCVREFERIDA A UN PROCEDIMIENTO PARA PREPARAR N-(6-(3-TERT-BUTIL-5-(2,4-DIOXO-3,4-DIHIDROPIRIMIDIN-1(2H)-IL)-2-METOXIFENIL)NAFTALEN-2-IL)METANSULFONAMIDA (COMPUESTO A) O UNA SAL DEL MISMO, QUE COMPRENDE SULFONAMIDAR EL COMPUESTO (5) MEDIANTE UN PRECURSOR DE CATALIZADOR DE METAL DE TRANSICION TAL COMO UN PRECURSOR DE CATALIZADOR DE PALADIO Y UN LIGANDO TAL COMO UNA FOSFINA, EN PRESENCIA DE UNA BASE TAL COMO CARBONATO DE CESIO, CARBONATO DE SODIO, ENTRE OTR
