KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Archive for January 28th, 2007

WO2007011065

Posted by kinasepro on January 28, 2007

Mitsubishi has an app covering the intermediates for their GSK3 Sanofi-Aventis stuff. I still think the spiro compounds are sexier, but the morpholines are further explored so here we have a pretty solid looking asymmetric method to make 2-aryl morpholines via CBS reduction:

FC1=CC=C(C(CCl)=O)C=C1 FC1=CC=C([C@H](O)CCl)C=C1
FC1=CC=C([C@H](O)CNCC2=CC=CC=C2)C=C1 FC1=CC=C([C@H](OC2)CN(CC3=CC=CC=C3)C2=O)C=C1
FC1=CC=C([C@H]2CN(CC3=CC=CC=C3)CCO2)C=C1 FC1=CC=C([C@H]2CNCCO2)C=C1
Route starts on page 79 example 1, 2 & 5 shown here.

Array might have something to say with how novel the approach is, y’know given how they sell the (rac) stuff?

Posted in GSK3, Mitsubishi, Sanofi-Aventis | 2 Comments »