3-氨基-4-甲基苯甲酸合成路线 （共 46 条）
反应条件
N-bromosuccinmide in N,N-dimethyl-formamide
T=0°C; 1.16667 h; Inert atmosphere;
参考文献
GREEN CROSS CORPORATION; LEE, Jinhwa; KIM, Jeongmin; LEE, Suk Ho; LEE, Junwon; SONG, Kwang-Seop; PARK, Eun-Jung; KIM, Min Ju; SEO, Hee Jeong; LEE, Sung-Han; SON, Eun Jung; KIM, Jong Yup; KANG, Suk Youn; KONG, Younggyu
Patent: WO2011/159067 A2, 2011 ;
Location in patent: Page/Page column 28 ;
WO 2011/159067 A2
反应条件
1: 1) sodium nitrite, aq. HCl 2) KI, CuI / 1) under 0 deg C 2) water, 2 h reflux
2: 100 percent / NaOH, CuI / H2O / 8 h / Heating
3: 99 percent / 1) lithium diisopropylamide / tetrahydrofuran; various solvent(s) / 1) -5 to -15 deg C, 40 min. 2) warming to 10 deg C, 3 h
4: 98 percent / polyphosphoric acid, water / 0.5 h / 140 °C
5: 1) ethyl chloroformate, triethylamine 2) sodium borohydride / 1) tetrahydrofuran, 5 deg C, 15 min.; 15 deg C, 45 min. 2) water, 40 deg C, 4 h; 20 deg C, 18 h
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参考文献
Hands; Marley; Skittrall; Wright
Journal of Heterocyclic Chemistry, 1986 , vol. 23, # 5 p. 1333 - 1337
反应条件
1: 98 percent / acetic acid
2: HNO3 / 0 °C
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参考文献
Clews, John; Curtis, Anthony D.M.; Malkin, Hugh
Tetrahedron, 2000 , vol. 56, # 44 p. 8735 - 8746
反应条件
1: 80 percent / Fe(SO3C6H4NO2)3*4.5H2O / H2SO4 / 4 h / 140 °C
2: diethyl ether
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参考文献
Gracheva, I.N.; Tochilkin, A.I.
Chemistry of Heterocyclic Compounds (New York, NY, United States), 1980 , vol. 16, # 3 p. 275 - 277
Khimiya Geterotsiklicheskikh Soedinenii, 1980 , vol. 16, # 3 p. 366 - 368
反应条件
1: N-bromosuccinmide / N,N-dimethyl-formamide / 1 h / 0 °C / Inert atmosphere
2: thionyl chloride / 15 h / 0 °C / Reflux; Inert atmosphere
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参考文献
PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, S.A.; PROUS, Josep R.; SERRADELL, Neus; MUÑOZ, Rosa; FLORES, Ramón; GARCÍA-DELGADO, Noemí
Patent: WO2013/45495 A1, 2013 ;
反应条件
1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine; methylamine in tetrahydrofuran; DMF (N,N-dimethyl-formamide)
T=54°C; 2 h;
参考文献
BRISTOL-MYERS SQUIBB COMPANY
Patent: WO2003/99820 A1, 2003 ;
Location in patent: Page 35; 36 ;
WO 03/099820 A1
