3-氨基-4-甲基噻吩-2-甲酸甲酯合成路线 （共 25 条）
反应条件
1.1: 150 °C 2.1: trichlorophosphate / 1 h / 100 °C 3.1: hydrogen; sodium acetate / 20 palladium(II) hydroxide on carbon / ethyl acetate; isopropyl alcohol / 2585.81 Torr 4.1: N-bromosuccinmide / tetrachloromethane / 1 h / Reflux 4.2: 1 h / Reflux View Scheme
参考文献
HANMI PHARM CO., LTD.; BAE, In Hwan; SON, Jung Beom; HAN, Sang Mi; KWAK, Eun Joo; KIM, Ho Seok; SONG, Ji Young; BYUN, Eun Young; JUN, Seung Ah; AHN, Young Gil; SUH, Kwee Hyun
Patent: WO2013/100632 A1, 2013 ;
反应条件
1.1: triethylamine / dichloromethane / 0.5 h
1.2: Reflux
1.3: Reflux
2.1: trichlorophosphate / 0.25 h / 180 °C / microwave
3.1: hydrogen; sodium acetate / 20 palladium(II) hydroxide on carbon / ethyl acetate / 62 h / 2844.39 Torr
4.1: dibenzoyl peroxide; N-bromosuccinmide / tetrachloromethane / 0.25 h / 100 °C / microwave
4.2: 0.08 h / 150 °C / microwave
5.1: aminosulfonic acid; potassium dihydrogenphosphate; sodium chlorite / water; tert-butyl alcohol; tetrahydrofuran / 0.5 h
View Scheme
参考文献
Arora, Nidhi; Chen, Shaoqing; Hermann, Johannes Cornelius; Kuglstatter, Adreas; Labadie, Sharada Shenvi; Lin, Clara Jeou Jen; Lucas, Matthew C.; Moore, Amy Geraldine; Papp, Eva; Talamas, Francisco Xavier; Wanner, Jutta; Zhai, Yansheng
Patent: US2012/15962 A1, 2012 ;
US 20120015962 A1
反应条件
1: 24 h / 200 °C
2: trichlorophosphate / N,N-dimethyl-formamide / 4 h / 110 °C
3: palladium(II) oxide hydrate; triethylamine; hydrogen / methanol / 5 h
4: N-bromosuccinmide; 2,2'-azo-bisisobutyronitrile / benzene / 2 h / 75 °C
View Scheme
参考文献
HANMI PHARM CO., LTD.; BAE, In Hwan; SON, Jung Beom; HAN, Sang Mi; KWAK, Eun Joo; KIM, Ho Seok; SONG, Ji Young; BYUN, Eun Young; JUN, Seung Ah; AHN, Young Gil; SUH, Kwee Hyun
Patent: WO2013/100632 A1, 2013 ;
反应条件
sodium bis(2-methoxyethoxy)aluminium dihydride in potassium hydroxide; toluene
参考文献
Sandoz Ltd.
Patent: US4472425 A1, 1984 ;
反应条件
1: formic acid With acetic anhydride
T=0°C;
2: 3-amino-4-methyl-2-thiophenecarboxylic acid methyl ester T=0 - 20°C; 4 h;
参考文献
Thrash, Thomas; Cabell, Larry A.; Lohse, Daniel; Budde, Raymond J.A.
Patent: US2006/4002 A1, 2006 ;
Location in patent: Page/Page column 11; 21; 23; 30; 31 ;
