3-(4-氯苯基磺酰基)-2-甲基-4-硝基-1H-吲哚合成路线 (共 4 条)
反应条件
1: 3-nitro-aniline With tert-butylhypochlorite in tetrahydrofuran
T=-78 - -65°C; 0.416667 h;
2: (4-chlorophenyl)thiomethyl methyl ketone in tetrahydrofuran
T=-65°C; 2 h;
3: With triethylamine in tetrahydrofuran
T=-65 - 20°C;
参考文献
ASTRAZENECA AB
Patent: WO2004/7451 A1, 2004 ;
Location in patent: Page 38 ;
WO 2004/007451 A1
反应条件
1: 3-nitro-aniline With tert-butylhypochlorite in tetrahydrofuran
T=-78 - -65°C; 0.416667 h;
2: (4-chlorophenyl)thiomethyl methyl ketone in tetrahydrofuran
T=-78 - -65°C; 2 h;
3: With hydrogenchloride; triethylamine
more than 3 stages;
参考文献
ASTRAZENECA AB
Patent: WO2004/106302 A1, 2004 ;
Location in patent: Page 25 ;
WO 2004/106302 A1
反应条件
1: 4,4'-dichlorodiphenyl disulfide With trichloroisocyanuric acid in ethyl acetate
T=20°C; 0.5 h;
2: 2-methyl-4-nitro-1H-indole in ethyl acetate
T=20°C; 0.666667 h; Product distribution / selectivity;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2006/75139 A2, 2006 ;
Location in patent: Page/Page column 5-6 ;
WO 2006/075139 A2
反应条件
sodium methylate in methanol
T=60 - 65°C; 3.5 h; Product distribution / selectivity;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2006/75139 A2, 2006 ;
Location in patent: Page/Page column 5 ;
WO 2006/075139 A2