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结构式
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
646519-88-2
合成路线
(共 7 条)
646519-88-2
→
反应条件
5408-74-2
5-乙基-2-乙烯基吡啶
+
105355-27-9
匹格列酮
+
74772-78-4
5-(4-羟基苄基)噻唑烷-2,4-二酮
反应条件
acetic acid; zinc in ethyl acetate T=25 - 35°C; 9 h; Product distribution / selectivity;
参考文献
CADILA HEALTHCARE LIMITED
Patent: WO2004/7490 A2, 2004 ;
Location in patent: Page 39 ;
646519-88-2
→
反应条件
5408-74-2
5-乙基-2-乙烯基吡啶
+
105355-27-9
匹格列酮
+
74772-78-4
5-(4-羟基苄基)噻唑烷-2,4-二酮
反应条件
acetic acid; zinc in ethyl acetate T=25 - 35°C; 9 h; Product distribution / selectivity;
参考文献
CADILA HEALTHCARE LIMITED
Patent: WO2004/7490 A2, 2004 ;
Location in patent: Page 39 ;
646519-88-2
→
反应条件
112529-15-4
盐酸吡格列酮
反应条件
1: zinc; acetic acid / 15 h / 25 - 30 °C 2: hydrogenchloride / water; ethanol View Scheme
参考文献
US2014/88127 A1, ;
646519-88-2
→
反应条件
144809-28-9
5-[[4-[2-(5-乙基-2-吡啶基)-乙氧基]苯基]亚甲基]-2,4-噻唑烷二酮
反应条件
1.1: zinc; acetic acid / 15 h / 25 - 30 °C 2.1: N-bromosuccinmide / tert-butyl alcohol; water / 1.5 h / 25 °C / |Large scale 2.2: 0.75 h / |Large scale 2.3: PEG 4000 / 17 h / 78 °C / |Large scale 3.1: pyrrolidine / methanol / 2 h / 50 - 55 °C / |Large scale 4.1: thionyl chloride / chloroform / 3 h / |Reflux 5.1: zinc; acetic acid / methanol / 15 h / 25 - 30 °C View Scheme
参考文献
Cadila Healthcare Limited; Pandey, Bipin; Lonray, Vidya Bhushan; Lohray, Braj Bhushan
Patent: US2014/88127 A1, 2014 ;
646519-88-2
→
反应条件
105355-27-9
匹格列酮
反应条件
ammonium chloride; acetic acid; zinc Product distribution / selectivity;
参考文献
Cadila Healthcare Limited; Pandey, Bipin; Lonray, Vidya Bhushan; Lohray, Braj Bhushan
Patent: US2014/88127 A1, 2014 ;
Location in patent: Page/Page column 0191 ;
646519-88-2
→
反应条件
5408-74-2
5-乙基-2-乙烯基吡啶
+
105355-27-9
匹格列酮
+
74772-78-4
5-(4-羟基苄基)噻唑烷-2,4-二酮
反应条件
acetic acid; zinc in ethyl acetate T=25 - 35°C; 9 h; Product distribution / selectivity;
参考文献
CADILA HEALTHCARE LIMITED
Patent: WO2004/7490 A2, 2004 ;
Location in patent: Page 39 ;
646519-88-2
→
反应条件
101931-00-4
5-{4-[2-(5-乙基-2-吡啶基)-2-羟基乙氧基]苄基}-1,3-噻唑烷-2,4-二酮
反应条件
1.1: zinc; acetic acid / 15 h / 25 - 30 °C 2.1: N-bromosuccinmide / tert-butyl alcohol; water / 1.5 h / 25 °C / |Large scale 2.2: 0.75 h / |Large scale 2.3: PEG 4000 / 17 h / 78 °C / |Large scale 3.1: pyrrolidine / methanol / 2 h / 50 - 55 °C / |Large scale 4.1: sodium tetrahydroborate; dmgH2; CoCl2.6H2O / water; N,N-dimethyl-formamide / 4 h / 65 - 85 °C / |Large scale View Scheme
参考文献
Cadila Healthcare Limited; Pandey, Bipin; Lonray, Vidya Bhushan; Lohray, Braj Bhushan
Patent: US2014/88127 A1, 2014 ;