盐酸西那卡塞合成路线图解
摘要
<正>盐酸西那卡塞(cinacalcet hydrochloride,1),化学名为N-[(1R)-1-(1-萘基)乙基]-3-[3-(三氟甲基)苯基]丙基-1-胺盐酸盐,是一种由美国 NPS 药物公司研发的拟钙剂。该药物通过激活甲状旁腺中的钙离子受体来抑制甲状旁腺激素的分泌,进而增强受体对血流中钙离子的敏感程度,达到降低血清钙离子浓度的作用~([1-2])。盐酸西那卡塞在体内吸收良好,生物利用度高,人服用 2～6 h 后达到最大血药浓度~([2]),
The five methods for synthesizing cinacalcet hydrochloride,that is the first calcimimetic for the treatment of the secondary hyperparathyroidism of patients w ith chronic kidney disease,w ere graphically summarized w ith 19 references.
The five methods for synthesizing cinacalcet hydrochloride,that is the first calcimimetic for the treatment of the secondary hyperparathyroidism of patients w ith chronic kidney disease,w ere graphically summarized w ith 19 references.
引文
[1] NEMETH E F,HEATON W H,MILLER M,et al.Pharmacodynamics of the type Ⅱ calcimimetic compound cinacalcet HCl[J].J Pharmacol Exp Ther,2004,308(2):627-635.
[2] HARRIS R Z,PADHI D,MARBURY T C,et al.Pharmacokinetics,pharmacodynamics,and safety of cinacalcet hydrochloride in hemodialysis patients at doses up to 200 mg once daily[J].Am J Kidney Dis,2004,44(6):1070-1076.
[3] 韩雪,张东亮,刘文虎.西那卡塞治疗继发性甲状旁腺功能亢进的新进展[J].北京医学,2011,(2):175-177.
[4] 李林羚,胡雪峰,杨玉雷,等.盐酸西那卡塞的工艺研究[J].中国新药杂志,2013,(7):834-836..
[5] 国药一心制药有限公司.一种西那卡塞的合成与精制方法:中国,103739500[P].2012-12-27.
[6] 李建其,王冠,张莉,等.西那卡塞的制备方法:中国,103274948[P].2013-05-27.
[7] van WAGENEN B C,MOE S T,BALANDRIN M F,et al.Calcium receptor-active compounds:US,6211244[P].2001-08-03.
[8] 林国良,韩杰,张利华,等.一种西那卡塞中间体的合成方法:中国,103664577[P].2012-09-06.
[9] CATOZZI N,COTARCA L,FOLETTO J,et al.Process for preparing cinacalcet hydrochloride:WO,2010094674[P].2010-08-26.
[10] CATOZZI N,COTARCA L,FOLETTO J,et al.Process for preparing cinacalcet:WO,2011029833[P].2011-03-17.
[11] 吴范宏,杨雪艳,汤才飞.一种西那卡塞的绿色合成方法:中国,101941911[P].2010-09-21.
[12] 吕会超,白雪松,邹江,等.一种高纯度盐酸西那卡塞的制备方法:中国,103044267[P].2012-12-06.
[13] 余建红,周武春,叶兵,等.盐酸西那卡塞及其中间体的合成方法:中国,104774134[P].2014-01-09.
[14] SZEKERES T,RPSI J,SZAB A,et al.Process for preparing intermediate compounds useful for the preparation of cinacalcet:WO,20100267988[P].2010-10-21.
[15] 胡锦平,胡国宜,郑建龙,等.间三氟甲基苯丙醇的制备方法:中国,104892356[P].2015-05-08.
[16] 胡键,董菁,施小新.盐酸西那卡塞的合成[J].中国医药工业杂志,2010,(7):488-490.
[17] 陈维,翁科杰,宋文芳,等.一种芳基丙酸衍生物的制备方法:中国,102079697[P].2009-11-27.
[18] 吕刚,李光勋,唐卓.一种制备盐酸西那卡塞的方法[J].合成化学,2016,24(6):537-539.
[2] HARRIS R Z,PADHI D,MARBURY T C,et al.Pharmacokinetics,pharmacodynamics,and safety of cinacalcet hydrochloride in hemodialysis patients at doses up to 200 mg once daily[J].Am J Kidney Dis,2004,44(6):1070-1076.
[3] 韩雪,张东亮,刘文虎.西那卡塞治疗继发性甲状旁腺功能亢进的新进展[J].北京医学,2011,(2):175-177.
[4] 李林羚,胡雪峰,杨玉雷,等.盐酸西那卡塞的工艺研究[J].中国新药杂志,2013,(7):834-836..
[5] 国药一心制药有限公司.一种西那卡塞的合成与精制方法:中国,103739500[P].2012-12-27.
[6] 李建其,王冠,张莉,等.西那卡塞的制备方法:中国,103274948[P].2013-05-27.
[7] van WAGENEN B C,MOE S T,BALANDRIN M F,et al.Calcium receptor-active compounds:US,6211244[P].2001-08-03.
[8] 林国良,韩杰,张利华,等.一种西那卡塞中间体的合成方法:中国,103664577[P].2012-09-06.
[9] CATOZZI N,COTARCA L,FOLETTO J,et al.Process for preparing cinacalcet hydrochloride:WO,2010094674[P].2010-08-26.
[10] CATOZZI N,COTARCA L,FOLETTO J,et al.Process for preparing cinacalcet:WO,2011029833[P].2011-03-17.
[11] 吴范宏,杨雪艳,汤才飞.一种西那卡塞的绿色合成方法:中国,101941911[P].2010-09-21.
[12] 吕会超,白雪松,邹江,等.一种高纯度盐酸西那卡塞的制备方法:中国,103044267[P].2012-12-06.
[13] 余建红,周武春,叶兵,等.盐酸西那卡塞及其中间体的合成方法:中国,104774134[P].2014-01-09.
[14] SZEKERES T,RPSI J,SZAB A,et al.Process for preparing intermediate compounds useful for the preparation of cinacalcet:WO,20100267988[P].2010-10-21.
[15] 胡锦平,胡国宜,郑建龙,等.间三氟甲基苯丙醇的制备方法:中国,104892356[P].2015-05-08.
[16] 胡键,董菁,施小新.盐酸西那卡塞的合成[J].中国医药工业杂志,2010,(7):488-490.
[17] 陈维,翁科杰,宋文芳,等.一种芳基丙酸衍生物的制备方法:中国,102079697[P].2009-11-27.
[18] 吕刚,李光勋,唐卓.一种制备盐酸西那卡塞的方法[J].合成化学,2016,24(6):537-539.