A practical synthesis of 3,4-diethoxybenzthioamide based on Friedel-Crafts reaction with potassium thiocyanate in methanesulfonic acid

被引:16
作者
Aki, S [1 ]
Fujioka, T [1 ]
Ishigami, M [1 ]
Minamikawa, J [1 ]
机构
[1] Otsuka Pharmaceut Co Ltd, Proc Res Lab, Tokushima Factory 2, Kawaguchi, Tokushima 7710182, Japan
关键词
D O I
10.1016/S0960-894X(02)00398-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of 3,4-diethoxybenzthioamide, the key intermediate for OPC-6535, is achieved by employing Friedel-Crafts reaction of 1,2-diethoxybenzene with potassium thiocyanate in methanesulfonic acid at ambient temperature. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2317 / 2320
页数:4
相关论文
共 27 条
[21]  
SCHEIBYE S, 1978, B SOC CHIM BELG, V87, P229
[22]   NOVEL 5-HT3 ANTAGONISTS - INDOLE OXADIAZOLES [J].
SWAIN, CJ ;
BAKER, R ;
KNEEN, C ;
MOSELEY, J ;
SAUNDERS, J ;
SEWARD, EM ;
STEVENSON, G ;
BEER, M ;
STANTON, J ;
WATLING, K .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (01) :140-151
[23]   A NEW SYNTHESIS OF ALIPHATIC AND AROMATIC THIOAMIDES FROM NITRILES [J].
TAYLOR, EC ;
ZOLTEWICZ, JA .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1960, 82 (10) :2656-2657
[24]  
UHLENDORF J, Patent No. 3128452
[25]   Microwave-accelerated solvent-free synthesis of thioketones, thiolactones, thioamides, thionoesters, and thioflavonoids [J].
Varma, RS ;
Kumar, D .
ORGANIC LETTERS, 1999, 1 (05) :697-700
[26]   STUDIES ON ORGANO-PHOSPHORUS COMPOUNDS .47. PREPARATION OF THIATED SYNTHONS OF AMIDES, LACTAMS AND IMIDES BY USE OF SOME NEW P-CONTAINING, S-CONTAINING REAGENTS [J].
YDE, B ;
YOUSIF, NM ;
PEDERSEN, U ;
THOMSEN, I ;
LAWESSON, SO .
TETRAHEDRON, 1984, 40 (11) :2047-2052
[27]  
Yu DT, [No title captured], Patent No. [US 6156776., 6156776]