Solubility of 2-amino-6-chloropurine in Mitsunobu solvents could be significantly improved after its exocyclic amino group is protected via N-tert-butoxycarbonylation.The bis-Boc protected 2-amino-6-chloropurine also ...Solubility of 2-amino-6-chloropurine in Mitsunobu solvents could be significantly improved after its exocyclic amino group is protected via N-tert-butoxycarbonylation.The bis-Boc protected 2-amino-6-chloropurine also shows excellent activity and N9 selectivity in the coupling with various alcohols by a Mitsunobu reaction.Then,a new practical and efficient method is established for the synthesis of penciclovir(PCV) from bis-Boc-2-amino-6-chloropurine 9 and the side chain of 5-(2-hydroxyethyl)-2,2-dimethyl-1,3-dioxane 5—the latter being a more easily prepared cyclic precursor of the diacetate side chain used in the conventional process.The coupling of 9 with 5 proceeded regioselectively at a N9 position of purine derivative for a good yield under Mitsunobu conditions.展开更多
目的:探究喷昔洛韦联合阿昔洛韦软膏治疗带状疱疹的疗效及患者疼痛、血清IL-2、IL-6水平变化情况。方法:选取2016年9月至2020年10月间本院收治的142例带状疱疹患者为研究对象,采用简单随机分组法分为观察组和对照组,71例/组。对照组采...目的:探究喷昔洛韦联合阿昔洛韦软膏治疗带状疱疹的疗效及患者疼痛、血清IL-2、IL-6水平变化情况。方法:选取2016年9月至2020年10月间本院收治的142例带状疱疹患者为研究对象,采用简单随机分组法分为观察组和对照组,71例/组。对照组采用常规软膏涂抹治疗,观察组在此基础上给予喷昔洛韦治疗。比较两组疗效、临床症状改善时间(带状疱疹结痂、水疱停止发展、疼痛消失时间);比较治疗前后两组患者神经痛评分(VAS);比较治疗前后两组血清炎症因子[白细胞介素-2(IL-2)、白细胞介素-6(IL-6)、白细胞介素-10(IL-10)]变化;比较治疗前后T细胞亚群[T淋巴细胞(T lymphocyte,CD3^(+))、辅助性T细胞(Helper T cells,CD4^(+))、细胞毒性T细胞(Cytotoxic T cells,CD8^(+))、CD4^(+)/CD8^(+)]变化;记录治疗期间不良反应发生率。结果:治疗7d后,观察组治疗有效率高于对照组(P<0.05);观察组临床症状改善时间均短于对照组(P<0.05);治疗后两组VAS评分均降低且观察组低于对照组(P<0.05);治疗后,两组IL-2、IL-10水平和CD3^(+)、CD4^(+)及CD4^(+)/CD8^(+)均升高,且观察组高于对照组(P<0.05);两组IL-6水平均下降,且观察组低于对照组(P<0.05)。治疗期间两组不良反应发生率无明显差异(P>0.05)。结论:喷昔洛韦联合阿昔洛韦软膏治疗带状疱疹的疗效显著,能缓解神经疼痛,缩短症状消退时间,调节炎症因子,提高免疫功能,且安全性高。展开更多
文摘Solubility of 2-amino-6-chloropurine in Mitsunobu solvents could be significantly improved after its exocyclic amino group is protected via N-tert-butoxycarbonylation.The bis-Boc protected 2-amino-6-chloropurine also shows excellent activity and N9 selectivity in the coupling with various alcohols by a Mitsunobu reaction.Then,a new practical and efficient method is established for the synthesis of penciclovir(PCV) from bis-Boc-2-amino-6-chloropurine 9 and the side chain of 5-(2-hydroxyethyl)-2,2-dimethyl-1,3-dioxane 5—the latter being a more easily prepared cyclic precursor of the diacetate side chain used in the conventional process.The coupling of 9 with 5 proceeded regioselectively at a N9 position of purine derivative for a good yield under Mitsunobu conditions.
文摘目的:探究喷昔洛韦联合阿昔洛韦软膏治疗带状疱疹的疗效及患者疼痛、血清IL-2、IL-6水平变化情况。方法:选取2016年9月至2020年10月间本院收治的142例带状疱疹患者为研究对象,采用简单随机分组法分为观察组和对照组,71例/组。对照组采用常规软膏涂抹治疗,观察组在此基础上给予喷昔洛韦治疗。比较两组疗效、临床症状改善时间(带状疱疹结痂、水疱停止发展、疼痛消失时间);比较治疗前后两组患者神经痛评分(VAS);比较治疗前后两组血清炎症因子[白细胞介素-2(IL-2)、白细胞介素-6(IL-6)、白细胞介素-10(IL-10)]变化;比较治疗前后T细胞亚群[T淋巴细胞(T lymphocyte,CD3^(+))、辅助性T细胞(Helper T cells,CD4^(+))、细胞毒性T细胞(Cytotoxic T cells,CD8^(+))、CD4^(+)/CD8^(+)]变化;记录治疗期间不良反应发生率。结果:治疗7d后,观察组治疗有效率高于对照组(P<0.05);观察组临床症状改善时间均短于对照组(P<0.05);治疗后两组VAS评分均降低且观察组低于对照组(P<0.05);治疗后,两组IL-2、IL-10水平和CD3^(+)、CD4^(+)及CD4^(+)/CD8^(+)均升高,且观察组高于对照组(P<0.05);两组IL-6水平均下降,且观察组低于对照组(P<0.05)。治疗期间两组不良反应发生率无明显差异(P>0.05)。结论:喷昔洛韦联合阿昔洛韦软膏治疗带状疱疹的疗效显著,能缓解神经疼痛,缩短症状消退时间,调节炎症因子,提高免疫功能,且安全性高。
