Ruchelman, Alexander L’s team published research in Tetrahedron: Asymmetry in 2015-05-31 | 608141-42-0

Tetrahedron: Asymmetry published new progress about Enantioselective synthesis. 608141-42-0 belongs to class ethers-buliding-blocks, and the molecular formula is C12H19NO4S, COA of Formula: C12H19NO4S.

Ruchelman, Alexander L.; Connolly, Terrence J. published the artcile< Enantioselective synthesis of the apremilast aminosulfone using catalytic asymmetric hydrogenation>, COA of Formula: C12H19NO4S, the main research area is enantioselective apremilast aminosulfone catalytic asym hydrogenation.

Celgene’s Otezla (apremilast) is the first and only PDE4 inhibitor approved by the US FDA for the treatment of plaque psoriasis and psoriatic arthritis. Apremilast has been historically prepared via resolution to obtain the enantioenriched aminosulfone intermediate. Herein we have investigated the use of catalytic asym. hydrogenation for the enantioselective synthesis of the key aminosulfone intermediate in order to identify a higher yielding and greener synthesis route. Asym. reduction of the enamine 3-EtO-4-MeOC6H3C(NH2):CHSO2Me and the ketone 3-EtO-4-MeOC6H3COCH2SO2Me both proceeded with high selectivities, generating their resp. products with >95% ee.

Tetrahedron: Asymmetry published new progress about Enantioselective synthesis. 608141-42-0 belongs to class ethers-buliding-blocks, and the molecular formula is C12H19NO4S, COA of Formula: C12H19NO4S.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem