1030837-49-0Relevant articles and documents
Practical asymmetric synthesis of an edivoxetine·HCl intermediate via an efficient diazotization process
Kopach, Michael E.,Heath, Perry C.,Scherer, Roger B.,Pietz, Mark A.,Astleford, Bret A.,McCauley, Mary Kay,Singh, Utpal K,Wong, Sze Wing,Coppert, David M.,Kerr, Mark S.,Houghton, Peter G.,Rhodes, Gary A.,Tharp, Gregg A.
, p. 543 - 550 (2015/04/27)
A convergent synthesis of (S)-(4-benzylmorpholin-2-yl)(morpholino)methanone methanesulfonate (1), a key regulatory starting material for edivoxetine·HCl, was developed at Eli Lilly & Company. This novel synthesis utilizes d-serine as the source of chirali
Enantioselective synthesis of (R)- and (S)-N-Boc-morpholine-2-carboxylic acids by enzyme-catalyzed kinetic resolution: application to the synthesis of reboxetine analogs
Fish, Paul V.,Mackenny, Malcolm,Bish, Gerwyn,Buxton, Timothy,Cave, Russell,Drouard, David,Hoople, David,Jessiman, Alan,Miller, Duncan,Pasquinet, Christelle,Patel, Bhairavi,Reeves, Keith,Ryckmans, Thomas,Skerten, Melanie,Wakenhut, Florian
scheme or table, p. 389 - 391 (2009/05/11)
The (R)- and (S)-N-Boc-morpholine-2-carboxylic acids 9 and 10 were prepared using an enantioselective synthesis employing a highly selective enzyme-catalyzed kinetic resolution of racemic n-butyl 4-benzylmorpholine-2-carboxylate (11) as the key step. Acids 9 and 10 were then converted efficiently and stereoselectively to reboxetine analogs 3 and 4.
