1-甲基-4-(2-丙炔磺酰基)-苯合成路线 （共 13 条）
反应条件
in diethyl ether; hexane N2 atmosphere; propargyl addn. to lithium carborane in hexane/ether (prepd. in situ), stirring (20°C), boiling (0.5 h); pouring into aq. HCl, petroleum ether, stirring, filtration, org. layerwashing (water), drying (over Na2SO4), solvent removal (vac.);
参考文献
Zakharkin, L. I.; Kovredov, A. I.; Shaugumbekova, Zh. S.; Vinogradova, L. E.; Leites, L. A.
Journal of General Chemistry USSR (English Translation), 1981 , vol. 51, p. 1343 - 1346
Zhurnal Obshchei Khimii, 1981 , vol. 51, p. 1582 - 1586
反应条件
water; p-toluidine in ethanol T=60°C; 1.5 h; oth. amine, oth. solvent; C2H5OH, HgSO4, 70 deg C, 4-5 h;
参考文献
Journal of Organic Chemistry USSR (English Translation), , vol. 24, # 9 p. 1756 - 1759
Zhurnal Organicheskoi Khimii, , vol. 24, # 9 p. 1948 - 1952
反应条件
1: propargyl alcohol With potassium hydroxide in ethylene glycol dimethyl ether
T=0°C; 0.5 h;
2: p-toluenesulfonyl chloride in ethylene glycol dimethyl ether
T=0°C; 4 h;
参考文献
PRESIDIO PHARMACEUTICALS, INC.; ZHONG, Min; LI, Leping
Patent: WO2012/58125 A1, 2012 ;
Location in patent: Page/Page column 181 ;
WO 2012/058125 A1
反应条件
pyridine in chloroform
T=25°C; 2 h; Irradiation;
参考文献
Gupta, B. Dass; Roy, Sujit
Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999), 1988 , p. 1377 - 1384
反应条件
pyridine in dichloromethane
T=10°C; 4 h; Irradiation; Yields of byproduct given;
参考文献
Gupta, B. Dass; Roy, Sujit
Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999), 1988 , p. 1377 - 1384
反应条件
1: (i) NaOEt, (ii) /BRN= 605309/
2: MCPBA / CH2Cl2
View Scheme
参考文献
Yoshimoto,M. et al.
Chemical and Pharmaceutical Bulletin, 1971 , vol. 19, p. 1409 - 1415
反应条件
1: 98 percent / Et3N / CH2Cl2 / 1.) -78 deg C, 2 h, 2.) 0 deg C, 1 h
2: 2,6-lutidine / acetonitrile / 6 h / Heating
View Scheme
参考文献
Linden, Johannes B. van der; Asten, Peter F. T. M. van; Braverman, Samuel; Zwanenburg, Binne
Recueil des Travaux Chimiques des Pays-Bas, 1995 , vol. 114, # 2 p. 51 - 60
反应条件
triphenylphosphine in benzene
参考文献
Nunez Jr., Alberto; Rosario Martin; Fraile, Alberto; Garcia Ruano, Jose L.
Chemistry - A European Journal, 2010 , vol. 16, # 18 p. 5443 - 5453
反应条件
2: aq. H2O2, AcOH
View Scheme
参考文献
Truce,W.E.; Markley,L.D.
Journal of Organic Chemistry, 1970 , vol. 35, # 10 p. 3275 - 3281
反应条件
triethylamine
Yield given;
参考文献
Mikhailova, V. N.; Bulat, A. D.; Yurevich, V. P.; Ezhova, L. A.
Journal of Organic Chemistry USSR (English Translation), 1988 , vol. 24, # 9 p. 1756 - 1759
Zhurnal Organicheskoi Khimii, 1988 , vol. 24, # 9 p. 1948 - 1952
