N-Boc-4-(4-甲苯磺酰氧基甲基)哌啶合成路线 （共 12 条）
反应条件
pyridine T=0 - 20°C; 16 h;
参考文献
Chiesi Farmaceutici S.p.A.; RANCATI, Fabio; Rizzi, Andrea; Linney, Ian; Blackaby, Wesley; Knight, Chris
Patent: US2013/34504 A1, 2013 ;
Location in patent: Paragraph 0147; 0148; 0149 ;
反应条件
in diethyl ether; tert-butyl methyl ether
参考文献
AstraZeneca AB
Patent: US7235559 B1, 2007 ;
US 7235559 B1
反应条件
in tetrahydrofuran; pyridine
参考文献
US5763458 A1, ;
US 5763458 A
反应条件
in diethyl ether; tert-butyl methyl ether
参考文献
US2004/48881 A1, ;
US 20040048881 A1
反应条件
2: 37.8 percent / triethylamine / CH2Cl2 View Scheme
参考文献
Journal of Labelled Compounds and Radiopharmaceuticals, , vol. 42, # 13 p. 1289 - 1300
反应条件
tetraethyl ammonium fluoride in acetonitrile T=70°C; Fluorination; 6 h;
参考文献
Gilissen; Bormans; De Groot; Verbruggen
Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # 13 p. 1289 - 1300
反应条件
1: 7-hydroxy-6-methoxy-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one With potassium carbonate in DMF (N,N-dimethyl-formamide) T=20°C; 0.5 h; 2: 1-(tert-butoxycarbonyl)-4-(4-methylphenylsulphonyloxymethyl)piperidine in DMF (N,N-dimethyl-formamide) T=100°C; 2 h;
参考文献
AstraZeneca AB
Patent: EP1119567 B1, 2005 ;
Location in patent: Page/Page column 45 ;
反应条件
potassium carbonate in N,N-dimethyl-formamide T=95°C; 2 h;
参考文献
AstraZeneca AB
Patent: EP1244647 B1, 2006 ;
Location in patent: Page/Page column 19 ;
EP 1244647 B1
反应条件
1: 4-(4-bromo-2-fluorophenylamino)-7-hydroxy-6-methoxyquinazoline With potassium carbonate in 1-methyl-pyrrolidin-2-one 0.166667 h; 2: 1-(tert-butoxycarbonyl)-4-(4-methylphenylsulphonyloxymethyl)piperidine in 1-methyl-pyrrolidin-2-one T=95°C; 3.5 - 4 h; Product distribution / selectivity;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2007/36713 A2, 2007 ;
Location in patent: Page/Page column 56; 57 ;
WO 2007/036713 A2
反应条件
1: 79 percent / K2CO3 / dimethylformamide / 2 h / 95 °C 2: 70 percent / TFA / CH2Cl2 / 1 h / 20 °C View Scheme
参考文献
Hennequin, Laurent F.; Stokes, Elaine S. E.; Thomas, Andrew P.; Johnstone, Craig; Ple, Patrick A.; Ogilvie, Donald J.; Dukes, Michael; Wedge, Stephen R.; Kendrew, Jane; Curwen, Jon O.
Journal of Medicinal Chemistry, 2002 , vol. 45, # 6 p. 1300 - 1312
