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5-(4-溴苯基)-4,6-二氯嘧啶与N-丙胺基磺酰胺钾盐发生胺化反应制得N-[5-(4-溴苯基)-6-氯-4-嘧啶基]-N’-丙胺基磺酰胺,在叔丁醇钾作用下与乙二醇发生醇解反应制得N-[5-(4-溴苯基)-6-(2-羟乙氧基)-4-嘧啶基]-N’-丙胺基磺酰胺,与5-溴-2-氯嘧啶发生缩合反应并经过甲醇精制得到马西替坦,总收率为66%。
N- [5- (4-Bromophenyl) -6-chloro-4-pyrimidin-4- - pyrimidinyl] -N’-propylaminosulfonamide was reacted with ethylene glycol in the presence of potassium tert-butoxide to give N- [5- (4-bromophenyl) -6- Oxy) -4-pyrimidinyl] -N’-propylaminosulfonamide was condensed with 5-bromo-2-chloropyrimidine and purified by methanol to give macitentan in a total yield of 66%.