Development of a Scalable Asymmetric Process for the Synthesis of GLYT1 Inhibitor BI 425809 (Iclepertin)

Author:

Frutos Rogelio1ORCID,Tampone Thomas G.1,Mulder Jason1ORCID,Gao Joe1,Sieber Joshua D.1ORCID,Rodriguez Sonia1ORCID,Haddad Nizar1ORCID,Baer Katrin1,Brown Jack1,Yang Bing-Shiou1,Giovannini Riccardo1,Song Jinhua J.1,Grinberg Nelu1,Lee Heewon1,Senanayake Chris H.1

Affiliation:

1. Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, Connecticut 06877-0368, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Reference15 articles.

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2. Giovannini, R.; Bertani, B.; Ferrara, M.; Lingard, I.; Mazzaferro, R.; Rosenbrock, H. Phenyl-3-Aza-Bicyclo[3.1.0]Hex-3-yl-Methanones and the use Thereof as Medicament. Patent WO 2013017657 A1, 2013.

3. Safety, Tolerability and Pharmacokinetics of Oral BI 425809, a Glycine Transporter 1 Inhibitor, in Healthy Male Volunteers: A Partially Randomised, Single-Blind, Placebo-Controlled, First-in-Human Study

4. Enantiomerically Pure Synthesis of β-Substituted γ-Butyrolactones:  A Key Intermediate to Concise Synthesis of Pregabalin

5. Alvaro, G.; Cardullo, F.; Castiglioni, E. Piperidine Based Ureas as NK1 Antagonists. Patent WO 2010007032 A1, 2010.

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