(R)-1-(1-萘基)乙胺合成路线 （共 75 条）
反应条件
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine in dichloromethane T=0 - 23°C; Combinatorial reaction / High throughput screening (HTS)Inert atmosphere;
参考文献
Ghosh, Arun K.; Takayama, Jun; Aubin, Yoann; Ratia, Kiira; Chaudhuri, Rima; Baez, Yahira; Sleeman, Katrina; Coughlin, Melissa; Nichols, Daniel B.; Mulhearn, Debbie C.; Prabhakar, Bellur S.; Baker, Susan C.; Johnson, Michael E.; Mesecar, Andrew D.
Journal of Medicinal Chemistry, 2009 , vol. 52, # 16 p. 5228 - 5240
反应条件
ammonia; hydrogen T=175°C; P=46504.7 - 50255 Torr; 12 h; Autoclave; Catalytic behavior; ConcentrationPressure;
参考文献
SCHREMS, Marcus Georg
Patent: US2013/345475 A1, 2013 ;
Location in patent: Paragraph 0117 ;
反应条件
ammonia; hydrogen T=200°C; P=46504.7 - 50255 Torr; 12 h; Autoclave; Catalytic behavior;
参考文献
SCHREMS, Marcus Georg
Patent: US2013/345475 A1, 2013 ;
Location in patent: Paragraph 0116 ;
反应条件
1: With [{(η5-C5Me5)IrCl}2(μ-Cl)2] in toluene T=110°C; 6 h; Inert atmosphere; 2: With hydrogenchloride in diethyl ether; hexane; ethyl acetate; toluene Reagent/catalystTime;
参考文献
ZENTIVA, K.S.; VLASAKOVA Ruzena; HAJICEK Josef
Patent: WO2013/75679 A1, 2013 ;
Location in patent: Page/Page column 9 ;
反应条件
1: (R)-(+)-1-(1-naphthyl)-ethylamine; benzaldehyde T=25 - 30°C; 2: 1-(3-bromopropyl)-3-(trifluoromethyl)benzene in 1-methyl-pyrrolidin-2-one T=130 - 140°C; 12 h; 3: With hydrogenchloride; water in 1-methyl-pyrrolidin-2-one; toluene pH=0.5 - 2;
参考文献
Amneal Pharmaceuticals, LLC
Patent: US2011/319663 A1, 2011 ;
Location in patent: Page/Page column 18 ;
反应条件
1: With sodium tetrahydroborate; boric acid T=20°C; 14.5 h; 2: With hydrogenchloride in hexane; water T=20°C; pH=1 - 3; 3.5 h;
参考文献
TYCHE INDUSTRIES LIMITED; NARAYANA, Rao Mutyala; RAMADAS, Chavakula; SRINIVASA, Rao Chennupati; SANDEEP, Gokaraju
Patent: WO2014/16847 A1, 2014 ;
Location in patent: Page/Page column 5; 9 ;
反应条件
1.1: potassium carbonate; potassium iodide / isopropyl alcohol / 4 h / 80 - 85 °C / Inert atmosphere 1.2: 1 h / 20 °C / Inert atmosphere 1.3: 20 °C / pH 11 - 12 / Inert atmosphere 2.1: iron acetylacetonate / 1-methyl-pyrrolidin-2-one; tetrahydrofuran / -30 - 0 °C / Inert atmosphere 2.2: 0.25 h / 10 - 35 °C / pH 0 - 1 / Inert atmosphere 3.1: sodium hydrogencarbonate / ethyl acetate; water / 1 h / 20 °C / Inert atmosphere 3.2: 1 h / 20 °C / Inert atmosphere 4.1: hydrogenchloride; hydrogen / 2-5percent w/w palladium on carbon / water; methanol / 20 - 30 °C / Inert atmosphere View Scheme
参考文献
RANBAXY LABORATORIES LIMITED; MUKHTAR, Sayeed; NAIR, Dinesh, Shashidharan; MEDHANE, Roshan, Ramesh; MAHESHWARI, Nitin; MEERAN, Hashim, Nizar, Poovanathil, Nagoor; TEWARI, Neera; PRASAD, Mohan
Patent: WO2011/33473 A1, 2011 ;
反应条件
1: (R)-(+)-1-(1-naphthyl)-ethylamine With benzaldehyde T=25 - 30°C; Forster reaction; 2: 1-(3-bromopropyl)-3-(trifluoromethyl)benzene in 1-methyl-pyrrolidin-2-one T=125 - 130°C; Forster reaction; Further stages;
参考文献
Shinde, Gorakshanath B.; Niphade, Navnath C.; Deshmukh, Shrikant P.; Toche, Raghunath B.; Mathad, Vijayavitthal T.
Organic Process Research and Development, 2011 , vol. 15, # 2 p. 455 - 461
反应条件
1: 96 percent / benzene / 2 h / Heating 2: BF3*Et2O / toluene; diethyl ether / 1.5 h / -78 °C 3: H2 / Pd(OH)2/C / methanol / 6 h / 20 °C View Scheme
参考文献
Gong, Yuefa; Kato, Katsuya
Tetrahedron Asymmetry, 2001 , vol. 12, # 15 p. 2121 - 2127
反应条件
ammonia; hydrogen T=200°C; P=46504.7 - 50255 Torr; 12 h; Autoclave; Catalytic behavior;
参考文献
SCHREMS, Marcus Georg
Patent: US2013/345475 A1, 2013 ;
Location in patent: Paragraph 0116 ;
