帕瑞昔布钠杂质整套作为一种手术后的短期止痛药,广泛用于临床术后缓解疼痛,该产品是辉瑞公司研发,其商品名是:特耐,其主要作用机理是:帕瑞昔布钠是伐地昔布的前体药物,伐地昔布在临床剂量范围是选择性环氧合酶-2(COX-2)YZ剂,而COX-2与疼痛、炎症和发热有关的前列腺素样递质的合成过程中发挥Z主要作用,但是其真正发挥作用的还是属于伐地昔布,但是由于伐地昔布在水中的溶解度不好,所以,在体外制备成帕瑞昔布钠,进入体内后,融化水解成伐地昔布,进而由伐地昔布主要发挥作用。
此外,帕瑞昔布钠的合成工艺,我司也摸索出来,主要是在合成的过程中,容易产生相关杂质,帕瑞昔布钠杂质1 5-methyl-3,4-diphenylisoxazole 37928-17-9
2 509074-26-4 4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonylchloride
3 4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonic acid 181696-35-5 4 4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonamide 181695-72-7 5 3-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonamide 386273-25-2 6 3-(5-methyl-4-phenylisoxazol-3-yl)benzenesulfonamide 1373038-56-2 7 4-(5-methyl-4-phenylisoxazol-3-yl)benzenesulfonamide 181696-12-8 8 3-(5-methyl-4-(4-sulfamoylphenyl)isoxazol-3-yl)benzenesulfonamide 1373038-59-5
8 3,3'-(5-methylisoxazole-3,4-diyl)dibenzenesulfonamide N/A检索至20170708
9 4-(5-methyl-3-phenylisoxazol-4-yl)-N-((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)benzenesulfonamide 1373038-60-8
昔布钠杂质15 N-((4-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)acetamide 198471-06-6 昔布钠杂质8 N-((3-(5-methyl-3-phenylisoxazol-4-yl)phenyl)sulfonyl)propionamide N/A检索至20170708
昔布钠杂质16 N-((3-(5-methyl-4-phenylisoxazol-3-yl)phenyl)sulfonyl)propionamide N/A检索至20170708
昔布钠杂质19 N-((4-(5-methyl-3-(3-(Npropionylsulfamoyl)phenyl)isoxazol-4-yl)phenyl)sulfonyl)propionamide
1708094-99-8
昔布钠杂质20 ethyl 4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonate 473465-11-1
另外在合成的过程中,应该注意:晶型,溶解度,溶度,熔点的控制,这样才能对药品Z后的LX有很好的把握,如果有关于相关的了解,张超 3001006472