Organic Process Research and Development p. 490 - 495 (2008)
Update date:2022-08-05
Topics:
Liu, Yi-Feng
Wang, Cui-Ling
Bai, Ya-Jun
Han, Ning
Jiao, Jun-Ping
Qi, Xiao-Li
Imatinib and its analogues were successfully synthesized by an improved method in 19.5-46.2% total yield of six main steps. Pyrimidinyl amine was prepared by the reaction of enaminone and guanidine nitrate without the use of a toxic cyanamide. N-(2-Methyl-5-nitrophenyl)-4-(pyridin-3-yl) pyrimidin-2-amine as a key intermediate for the synthesis of imatinib was prepared by coppercatalyzed iV-arylation of heteroarylamme in 82% yield. The copper salts were used instead of the expensive palladium compounds in this C-N bond-forming reaction. The intermediate nitro compound was reduced by a N2H 4.H2O/FeCl3/C system using water as a solvent in good yield.
View MoreShanghai Harvest Chemical Ind. Co., Ltd.
Contact:021-51385350
Address:ROOM 806-807, AI LI CHEN BUILDING, No.333 JINGXIANG ROAD, PUDONG DISTRICT, 201206, SHANGHAI
Taizhou volsen chemical Co., Ltd
website:http://www.volsenchem.com
Contact:+86-576-88869393
Address:Jiaojiang District, Taizhou, Zhejiang, China.
website:http://www.win-winchemical.com
Contact:0086-577-64498589
Address:6F, No. 396 Xingping Road, Longwan Industrial Zone, Wenzhou City, Zhejiang, 325000 P.R.China
Contact:+44 7958 511245
Address:PO Box 469, Manchester, UK
SHANGHAI T&W PHARMACEUTICAL CO., LTD.
website:http://www.trustwe.com
Contact:+86-21-61551611
Address:601, No. 1, 2277 Nong, Zu Chongzhi Road, Zhangjiang Hightech. Park, Pudong
Doi:10.1016/j.tet.2007.11.080
(2008)Doi:10.1021/ja7114844
(2008)Doi:10.1007/s11164-010-0135-4
(2010)Doi:10.1021/ja00269a042
(1986)Doi:10.1055/s-2007-1000831
(2008)Doi:10.1002/ejoc.201500815
(2015)