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A Next Generation Synthesis of BACE1 Inhibitor Verubecestat (MK-8931).
- Source :
-
Organic letters [Org Lett] 2018 Mar 16; Vol. 20 (6), pp. 1568-1571. Date of Electronic Publication: 2018 Feb 26. - Publication Year :
- 2018
-
Abstract
- The development of a commercial manufacturing route to verubecestat (MK-8931) is described, highlights of which include the application of a continuous processing step to outcompete fast proton transfer in a Mannich-type ketimine addition, a copper-catalyzed amidation reaction, and an optimized guanidinylation procedure to form the key iminothiadiazine dioxide core.
Details
- Language :
- English
- ISSN :
- 1523-7052
- Volume :
- 20
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Organic letters
- Publication Type :
- Academic Journal
- Accession number :
- 29481097
- Full Text :
- https://doi.org/10.1021/acs.orglett.8b00259