Linagliptin

CAT#: H300125

CAS#: 668270-12-0

Description: Linagliptin, also known as BI-1356, is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes. Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly.

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Synthetic Routes

Linagliptin - Synthetic Route 1

Linagliptin route01

Synthetic reference

Eckhardt, Matthias; Langkopf, Elke; Mark, Michael; Tadayyon, Moh; Thomas, Leo; Nar, Herbert; Pfrengle, Waldemar; Guth, Brian; Lotz, Ralf; Sieger, Peter; Fuchs, Holger; Himmelsbach, Frank. 8-​(3-​(R)​-​Aminopiperidin-​1-​yl)​-​7-​but-​2-​ynyl-​3-​methyl-​1-​(4-​methyl-​quinazolin-​2-​ylmethyl)​-​3,​7-​dihydropurine-​2,​6-​dione (BI 1356)​, a Highly Potent, Selective, Long-​Acting, and Orally Bioavailable DPP-​4 Inhibitor for the Treatment of Type 2 Diabetes. Journal of Medicinal Chemistry. Volume 50. Issue 26. Pages 6450-6453. Journal. (2007).

Linagliptin - Synthetic Route 2

Linagliptin route02

Synthetic reference

Lin, Kuaile; Cai, Zhengyan; Wang, Fei; Zhang, Wei; Zhou, Weicheng. Synthesis and biological evaluation of xanthine derivatives on dipeptidyl peptidase 4. Chemical & Pharmaceutical Bulletin. Volume 61. Issue 4. Pages 477-482. Journal. (2013).

Linagliptin - Synthetic Route 3

Linagliptin route03

Synthetic reference

Huang, Yiwen; Lu, Hui; Zhang, Fuli; Min, Chunyan. Identification, isolation, characterization, and UHPLC quantification of potential genotoxic impurities in linagliptin. Journal of Separation Science. Volume 41. Issue 21. Pages 3985-3994. Journal; Online Computer File. (2018).

Linagliptin - Synthetic Route 4

Linagliptin route04

Synthetic reference

Dong, Weitong; Huang, Yao; Su, Shengmin; Sun, Yongfen; Zhang, Pengtao. Process for the preparation of a xanthine-based compound. Assignee Boehringer Ingelheim International GmbH, Germany. WO 2016207364. (2016).

Linagliptin - Synthetic Route 5

Linagliptin route05

Synthetic reference

Cao, Huanyan; Zhang, Haijun; Wu, Jiaquan; Zhang, Liang; Gao, Xuan. Preparation of intermediate for synthesizing linagliptin. Assignee Biortus Biosciences Co., Ltd., Peop. Rep. China. CN 105801580. (2016).

Linagliptin - Synthetic Route 6

Linagliptin route06

Synthetic reference

Tang, Tiansheng; Li, Fangling; Lu, Zhaoqiang; Ren, Peng; Shang, Wanli; Zhang, Yanjun. Intermediate of linagliptin and preparation method and application thereof. Assignee Shenzhen Haibin Pharmaceutical Co., Ltd., Peop. Rep. China; Xinxiang Haibin Pharmaceutical Co., Ltd. CN 104892609. (2015).