Development of a Scalable Synthesis of (S)-3-Fluoromethyl-γ-butyrolactone, Building Block for Carmegliptin’s Lactam Moiety

Author:

Adam Jean-Michel1,Foricher Joseph1,Hanlon Steven1,Lohri Bruno1,Moine Gérard1,Schmid Rudolf1,Stahr Helmut1,Weber Martin1,Wirz Beat1,Zutter Ulrich1

Affiliation:

1. F. Hoffmann-La Roche Ltd., Pharmaceuticals Division, †pRED, Pharma Research and Early Development, Process Research and Synthesis, and ‡Pharma Technical Development Actives, Grenzacherstrasse 124, CH-4070 Basel, Switzerland

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Reference46 articles.

1. Discovery of carmegliptin: A potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

2. Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors

3. An Efficient Process for the Manufacture of Carmegliptin

4. aAbrecht, S.; Adam, J.M.; Fettes, A.; Foricher, J.; Lohri, B.; Mattei, P.; Moine, G.; Schmid, R.; Zutter, U.(F. Hoffmann-La Roche AG). PCT Int. Appl. WO 2006/125728 A1, 2006.

5. bZutter, U.(F. Hoffmann-La Roche Inc.). U.S. Pat. Appl. Publ. U.S. 2008/108816 A1, 2008.

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