1005450-55-4

基本信息
西那卡塞雜質(zhì)13
西那卡塞雜質(zhì)24
西那卡塞雜質(zhì)117
鹽酸西那卡塞胺化物
N-[1-(R)-(1-萘基)乙基]-3-[3-三氟甲基苯基]丙酰胺
3-(3-三氟甲基-苯基)-N-(R)-(1-萘基-1-乙基)-丙酰胺
(R)-N-(1-(萘-1-基)乙基)-3-(3-(三氟甲基)苯基)丙酰胺
鹽酸西那卡塞/ 3-(3-三氟甲基-苯基)-N-(R)-(1-萘基-1-乙基)-丙酰胺
Cinacalcet Impurity 117
-N-(1-(Naphthalen-1-yl)
Cinacalcet Impurity 31/Cinacalcet amide Impurity)
N-((R)-1-(naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)pheny...
N-[1-(R)-(1-Naphthyl)ethyl]-3-[3-trifluoroMethylphenyl]propanaMide
(R)-N-(1-(phthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propamide
N-[1-(R)-(1-Naphthyl)ethyl]-3-[3-(trifluoromethyl)phenyl]-1-propanamide
N-《R)-I-(naphthalen-I-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propanamide
Benzenepropanamide, N-[(1R)-1-(1-naphthalenyl)ethyl]-3-(trifluoromethyl)-
物理化學性質(zhì)
制備方法

1095393-66-0

1005450-55-4
在另一種合成方案中,(E)-N-((R)-1-萘-1-基乙基)-3-(3-三氟甲基苯基)丙烯酰胺的雙鍵和酰胺羰基的還原采用分步法進行。可以選擇先還原羰基或烯烴雙鍵。以烯烴雙鍵的還原為例,反應在金屬催化劑存在下通過氫化實現(xiàn)。具體操作如下:將(E)-N-((R)-1-萘-1-基乙基)-3-(3-三氟甲基苯基)丙烯酰胺(1.0當量;0.67 mmol;250 mg)與10 wt% Pd/C(25 mg)在甲醇和甲苯(7 mL/1 mL)的混合溶劑中懸浮。反應燒瓶經(jīng)抽真空后,用氫氣氣球回填(重復三次)。反應混合物在室溫下攪拌,反應進程通過高效液相色譜(HPLC)監(jiān)測。90分鐘后,反應混合物通過硅藻土床過濾,濾液中的溶劑在真空下移除。所得固體在45℃的真空烘箱中干燥過夜。分離產(chǎn)率為91.2%(229 mg)。產(chǎn)物的結(jié)構(gòu)通過1H NMR和質(zhì)譜確認。1H NMR(400 MHz, CDCl3)δ ppm: 1.6(d, 3H), 2.39-2.53(m, 2H), 2.96-3.13(m, 2H), 5.55(br.s, 1H), 5.87-5.96(m, 1H), 7.29-7.38(m, 2H), 7.39-7.46(m, 4H), 7.46-7.55(m, 2H), 7.76-7.82(m, 1H), 7.83-7.89(m, 1H), 8.00-8.07(m, 1H)。高分辨質(zhì)譜(HRMS)(M+1): 372.1。
參考文獻:
[1] Patent: WO2009/2427, 2008, A2. Location in patent: Page/Page column 39
[2] Patent: WO2008/58235, 2008, A2. Location in patent: Page/Page column 34
[3] Patent: EP1990333, 2008, A1. Location in patent: Page/Page column 12