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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
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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-A
合成路线
（共 15 条）
1351564-28-7
→
反应条件
823817-56-7
西他列汀-A
反应条件
1: With hydrogenchloride; zinc in methanol; water T=20°C; 0.5 h; 2: With sodium hydroxide in water pH=10;
参考文献
LEK Pharmaceuticals d.d.
Patent: EP2392575 A1, 2011 ;
Location in patent: Page/Page column 36 ;
847445-81-2
3-氨基-1-[5,6-二氢-3-(三氟甲基)-1,2,4-噻唑并[4,3-a]吡嗪-7(8H)-基]-4-(2,4,5-三氟苯基)-2-丁烯-1-酮
→
反应条件
823817-56-7
西他列汀-A
反应条件
1: With methanesulfonic acid; dimethylsulfide borane complex in tetrahydrofuran; isopropyl alcohol T=-10 - -5°C; 4 h; 2: With ammonium hydroxide in tetrahydrofuran; water; isopropyl alcohol Product distribution / selectivity;
参考文献
CADILA HEALTHCARE LIMITED
Patent: US2011/213149 A1, 2011 ;
Location in patent: Page/Page column 15 ;
1253056-14-2
→
反应条件
823817-56-7
西他列汀-A
反应条件
methylamine in water; toluene T=25 - 40°C;
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; ESWARAIAH, Sajja; SATYANARAYANA, Revu; KONDAL REDDY, Bairy; SRINIVAS, Aluru
Patent: WO2010/122578 A2, 2010 ;
Location in patent: Page/Page column 67 ;
847445-81-2
3-氨基-1-[5,6-二氢-3-(三氟甲基)-1,2,4-噻唑并[4,3-a]吡嗪-7(8H)-基]-4-(2,4,5-三氟苯基)-2-丁烯-1-酮
→
反应条件
823817-56-7
西他列汀-A
+
1253056-01-7
反应条件
sodium tetrahydroborate; methanesulfonic acid in tetrahydrofuran; isopropyl alcohol T=-5 - 5°C;
参考文献
CADILA HEALTHCARE LIMITED; KOTHARI, Himanshu, Madhusudan; DAVE, Mayank, Ghanshyambhai; PANDEY, Bipin; SHUKLA, Bhavin, Shriprasad
Patent: WO2010/32264 A2, 2010 ;
Location in patent: Page/Page column 62 ;
1253056-15-3
→
反应条件
823817-56-7
西他列汀-A
反应条件
ammonium chloride; zinc in methanol Reflux;
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; ESWARAIAH, Sajja; SATYANARAYANA, Revu; KONDAL REDDY, Bairy; SRINIVAS, Aluru
Patent: WO2010/122578 A2, 2010 ;
Location in patent: Page/Page column 67 ;
767340-03-4
(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氢-[1,2,4]三唑并[4,3-a]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)丁-2-烯-2-胺
→
反应条件
823817-56-7
西他列汀-A
反应条件
sodium tetrahydroborate; acetic acid in toluene T=5 - 10°C; 3 h; Product distribution / selectivity;
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; ESWARAIAH, Sajja; SATYANARAYANA, Revu; KONDAL REDDY, Bairy; SRINIVAS, Aluru
Patent: WO2010/122578 A2, 2010 ;
Location in patent: Page/Page column 53 ;
209995-38-0
2,4,5-三氟苯乙酸
→
反应条件
823817-56-7
西他列汀-A
反应条件
1.1: 4-(N,N-dimethlyamino)pyridine / acetonitrile / 25 - 30 °C 1.2: 30 - 50 °C 2.1: ammonium hydroxide; ammonium acetate; acetic acid / water; methanol / 6 h / 60 - 65 °C 3.1: dimethylsulfide borane complex; methanesulfonic acid / isopropyl alcohol; tetrahydrofuran / 4 h / -10 - -5 °C View Scheme
参考文献
CADILA HEALTHCARE LIMITED
Patent: US2011/213149 A1, 2011 ;
1351564-26-5
→
反应条件
823817-56-7
西他列汀-A
反应条件
1.1: methanesulfonyl chloride; pyridine / 4 h / 20 °C 2.1: sodium tetrahydroborate / isopropyl alcohol; tetrahydrofuran / 3 h / 0 °C 2.3: pH 8 3.1: hydrogenchloride; zinc / water; methanol / 0.5 h / 20 °C 3.2: pH 10 View Scheme
参考文献
LEK PHARMACEUTICALS D.D.; STERK, Damjan; USTAR, Matjaz; ZLICAR, Marko
Patent: WO2011/151443 A1, 2011 ;
1351564-27-6
→
反应条件
823817-56-7
西他列汀-A
反应条件
1.1: sodium tetrahydroborate / isopropyl alcohol; tetrahydrofuran / 3 h / 0 °C 1.3: pH 8 2.1: hydrogenchloride; zinc / water; methanol / 0.5 h / 20 °C 2.2: pH 10 View Scheme
参考文献
LEK PHARMACEUTICALS D.D.; STERK, Damjan; USTAR, Matjaz; ZLICAR, Marko
Patent: WO2011/151443 A1, 2011 ;
1433546-53-2
→
反应条件
823817-56-7
西他列汀-A
反应条件
1: sodium azide / dimethyl sulfoxide / 27 h / 24 - 30 °C 2: hydrogen; 5 palladium on charcoal; sodium tetrahydroborate; methanol / 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 ;
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