The synthesis of S 18986, a chiral AMPA receptor modulator, via catalytic asymmetric hydrogenation

被引:32
作者
Cobley, CJ
Foucher, E
Lecouve, JP
Lennon, IC
Ramsden, JA
Thominot, G
机构
[1] Dow Chem Co USA, Chirotech Technol Ltd, Dowpharma, Cambridge CB4 0WG, England
[2] Oril Ind, Bolbec, France
关键词
D O I
10.1016/S0957-4166(03)00547-0
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The asymmetric hydrogenation of a dihydropyrrolo-benzothiadiazine dioxide 1 with a diphosphine ruthenium diamine catalyst has been used to synthesize the AMPA receptor positive modulator tetrahydropyrrolo-benzothiadiazine dioxide 2 (S 18986) in high enantiomeric excess. The use of factorial experimental design led to significant improvements in the process parameters and improved enantioselectivity. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3431 / 3433
页数:3
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