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乙二醇
甲醛
63148-62-9
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二甲基亚砜
碳酸氢钠
471-34-1
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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
西他列汀
合成路线
（共 81 条）
1433545-80-2
→
反应条件
486460-32-6
西他列汀
反应条件
1: sodium azide / dimethyl sulfoxide / 22 h / 20 - 30 °C 2: hydrogen; 5 palladium on charcoal; sodium tetrahydroborate; methanol / 42 h / 0 - 30 °C View Scheme
参考文献
CADILA HEALTHCARE LIMITED; PANDEY, Bipin; DAVE, Mayank, Ghanshyambhai; KOTHARI, Himanshu, M.; SHUKLA, Bhavin, Shriprasad; MENDIRATTA, Sanjeev, Kumar; JOSHI, Rupal; TRIVEDI, Umang
Patent: WO2013/65066 A1, 2013 ;
1152439-74-1
→
反应条件
486460-32-6
西他列汀
反应条件
1: sodium hydroxide; water / tetrahydrofuran / 5 h / 0 - 25 °C 2: CDI / ethyl acetate / 15 h / 50 - 55 °C 3: hydrogenchloride / water; isopropyl alcohol / 5 h / 20 - 55 °C View Scheme
参考文献
SMILAX LABORATORIES LIMITED; MALLELA, Sambhu, Prasad, Sarma; HAVALE, Shrikant, Hanumantappa; BODDEPALLI, Nagabhushana, Rao; GUNJI, Nagarjuna; MOKKAPATI, Bhavani, Sankar
Patent: WO2013/114173 A1, 2013 ;
1380243-28-6
→
反应条件
486460-32-6
西他列汀
反应条件
1: methyl iodide; water / methanol / 0.5 h / 20 °C / |Cooling with ice 2: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; sodium hypochlorite; sodium bromide; sodium hydrogencarbonate / dichloromethane / 2 h / 0 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; triethylamine / acetonitrile / 24 h / 0 - 20 °C 4: hydrogenchloride / water; methanol View Scheme
参考文献
Zhejiang Hisoar Pharmaceutical Co., Ltd; PAN, Xianhua; LI, Weijin; ZHANG, Qunhui; RUAN, Libo; YU, Wansheng; DENG, Fei; MA, Tianhua; HUANG, Mingwang; HE, Minhuan
Patent: EP2647624 A1, 2013 ;
1380243-35-5
→
反应条件
486460-32-6
西他列汀
反应条件
1: tetrabutyl ammonium fluoride / tetrahydrofuran / 2 h / 20 °C 2: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; sodium hypochlorite; sodium bromide; sodium hydrogencarbonate / dichloromethane / 2 h / 0 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; triethylamine / acetonitrile / 24 h / 0 - 20 °C 4: hydrogenchloride / water; methanol View Scheme
参考文献
Zhejiang Hisoar Pharmaceutical Co., Ltd; PAN, Xianhua; LI, Weijin; ZHANG, Qunhui; RUAN, Libo; YU, Wansheng; DENG, Fei; MA, Tianhua; HUANG, Mingwang; HE, Minhuan
Patent: EP2647624 A1, 2013 ;
1380243-37-7
→
反应条件
486460-32-6
西他列汀
反应条件
1: acetic acid / dichloromethane / 2 h / 20 °C 2: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; sodium hypochlorite; sodium bromide; sodium hydrogencarbonate / dichloromethane / 2 h / 0 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; triethylamine / acetonitrile / 24 h / 0 - 20 °C 4: hydrogenchloride / water; methanol View Scheme
参考文献
Zhejiang Hisoar Pharmaceutical Co., Ltd; PAN, Xianhua; LI, Weijin; ZHANG, Qunhui; RUAN, Libo; YU, Wansheng; DENG, Fei; MA, Tianhua; HUANG, Mingwang; HE, Minhuan
Patent: EP2647624 A1, 2013 ;
1380243-39-9
→
反应条件
486460-32-6
西他列汀
反应条件
1: palladium 10 on activated carbon; hydrogen / 12 h / 4560.31 Torr 2: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; sodium hypochlorite; sodium bromide; sodium hydrogencarbonate / dichloromethane / 2 h / 0 °C 3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; triethylamine / acetonitrile / 24 h / 0 - 20 °C 4: hydrogenchloride / water; methanol View Scheme
参考文献
Zhejiang Hisoar Pharmaceutical Co., Ltd; PAN, Xianhua; LI, Weijin; ZHANG, Qunhui; RUAN, Libo; YU, Wansheng; DENG, Fei; MA, Tianhua; HUANG, Mingwang; HE, Minhuan
Patent: EP2647624 A1, 2013 ;
1380243-41-3
→
反应条件
486460-32-6
西他列汀
反应条件
1.1: hydrogen; 20 palladium(II) hydroxide on carbon / methanol / 12 h / 50 °C / 4560.31 Torr / |Autoclave 1.2: 8 h / 20 °C 2.1: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; sodium hypochlorite; sodium bromide; sodium hydrogencarbonate / dichloromethane / 2 h / 0 °C 3.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; triethylamine / acetonitrile / 24 h / 0 - 20 °C 4.1: hydrogenchloride / water; methanol View Scheme
参考文献
Zhejiang Hisoar Pharmaceutical Co., Ltd; PAN, Xianhua; LI, Weijin; ZHANG, Qunhui; RUAN, Libo; YU, Wansheng; DENG, Fei; MA, Tianhua; HUANG, Mingwang; HE, Minhuan
Patent: EP2647624 A1, 2013 ;
1048703-14-5
→
反应条件
486460-32-6
西他列汀
反应条件
1: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; sodium hypochlorite; sodium bromide; sodium hydrogencarbonate / dichloromethane / 2 h / 0 °C 2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; triethylamine / acetonitrile / 24 h / 0 - 20 °C 3: hydrogenchloride / water; methanol View Scheme
参考文献
Zhejiang Hisoar Pharmaceutical Co., Ltd; PAN, Xianhua; LI, Weijin; ZHANG, Qunhui; RUAN, Libo; YU, Wansheng; DENG, Fei; MA, Tianhua; HUANG, Mingwang; HE, Minhuan
Patent: EP2647624 A1, 2013 ;
767352-30-7
(4R)-1-苯甲氧基-4-[(2,4,5-三氟苯基)甲基]-2-氮杂环丁酮
→
反应条件
486460-32-6
西他列汀
反应条件
1.1: lithium hydroxide hydrate / tetrahydrofuran; water / 2.33 h / 20 - 25 °C / pH 3 1.2: 3 h / 0 - 5 °C 2.1: phosphoric acid / isopropyl alcohol / 16 h / 30 °C 3.1: sodium hydroxide / water / 1 h / 0 - 5 °C View Scheme
参考文献
Sathe, Dhananjay Govind; Damle, Subhash Vishwanath; Arote, Nitin Dnyaneshwar; Ambre, Rakesh Ramchandra; Want, Kamlesh Digambar; Naik, Tushar Anil
Patent: US2013/158265 A1, 2013 ;
1352613-31-0
→
反应条件
486460-32-6
西他列汀
反应条件
1: sodium azide / N,N-dimethyl-formamide / 22 h / 25 - 42 °C 2: 5 palladium on charcoal; sodium tetrahydroborate / methanol / 42 h / 0 - 30 °C View Scheme
参考文献
CADILA HEALTHCARE LIMITED; Mendirata, Sanjeev Kumar; Pandey, Bipin; Joshi, Rupal; Trivedi, Umang; Dave, Mayank G.; Kothari, Himanshu M.; Shukla, Bhavin
Patent: US2013/289276 A1, 2013 ;
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