摘要
用1,2-二苯乙酮为原料,与氯磺酸反应得1-苯基-2-(4-磺酸基苯基)乙酮,在吡啶作用下与乙酰氯缩合制得1-苯基-2-(4-磺酸基苯基)-2-乙酰基乙酮,与盐酸羟胺环合得4-(5-甲基-3-苯基异噁唑-4-基)苯磺酸,经氯化、氨解制得伐地昔布,最后与丙酸酐反应制得帕瑞昔布,总收率约23%。
Parecoxib was synthesized from 1,2-diphenylethanone by reaction with chlorosulfonic acid, condensation with acetyl chloride in the presence of pyridine and cyclization with hydroxylamine hydrochloride to give 4-（5-methyl-3-phenylisoxazol-4-yl）phenylsulfonic acid, which was subjected to chlorination and ammonolysis to afford valdecoxib, followed by reaction with propionic anhydride with an overall yield of about 23%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第12期1207-1209,共3页
Chinese Journal of Pharmaceuticals
