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Ticagrelor

CAT#: H300147

CAS#: 274693-27-5

Description: Ticagrelor, also known as AZD-6140 and AR-C 126532XX, is a platelet aggregation inhibitor produced by AstraZeneca. The drug was approved in 2011. Ticagrelor is an antagonist of the P2Y12 receptor. Like the thienopyridines prasugrel, clopidogrel and ticlopidine, ticagrelor blocks adenosine diphosphate (ADP) receptors of subtype P2Y12. In contrast to the other antiplatelet drugs, ticagrelor has a binding site different from ADP, making it an allosteric antagonist, and the blockage is reversible. Moreover, the drug does not need hepatic activation, which might work better for patients with genetic variants regarding the enzyme CYP2C19.

Synthetic Routes

Ticagrelor - Synthetic Route 1

Synthetic reference

Zhang, Hao; Liu, Jun; Zhang, Luyong; Kong, Lingyi; Yao, Hequan; Sun, Hongbin. Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents. Bioorganic & Medicinal Chemistry Letters. Volume 22. Issue 11. Pages 3598-3602. Journal; Online Computer File. (2012).

Ticagrelor - Synthetic Route 2

Synthetic reference

Shimpi, Nitin A.; Prathi, Siva Koteswararao; Ponnuru, Anil Kumar; Batharaju, Ramesh; Dhake, Rajesh B. Novel synthetic methodology for the synthesis of Ticagrelor. Journal of Chemical and Pharmaceutical Research. Volume 8. Issue 1. Pages 797-803. Journal; Online Computer File. (2016).

Ticagrelor - Synthetic Route 3

Synthetic reference

Anon. Crystalline intermediates of (1S, 2S, 3R, 5S)-3-[7-[[(1R, 2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5,d]pyrimidine-3-yl]-5-(2-hydroxyethoxy)-1,2-cyclopentanediol. IP.com Journal. Volume 13. Issue 6A. Pages 1-19. Journal; Patent. (2013).

Ticagrelor - Synthetic Route 4

Synthetic reference

Canevotti, Renato; Della Negra, Federico; Mormile, Francesco; Previtali, Massimo; Rencurosi, Anna. Process for the preparation of triazolo[4,5-d]pyrimidinecyclopentane compounds. Assignee Flamma SpA, Italy. IT 1424427. (2016).

Ticagrelor - Synthetic Route 5

Synthetic reference

Rasadia, Punitkumar Rameshbhai; Ramani, Vaibhav Narendrakumar; Shah, Anamik Kantilal; Pandey, Bipin. Processes for preparing triazolo-[4,5-d]-pyrimidines, including ticagrelor, via coupling of amines with nucleobases. Assignee Anlon Chemical Research Organization, India. IN 2014MU01457. (2015).

Ticagrelor - Synthetic Route 6

Synthetic reference

She, Yang. Synthetic method of Ticagrelor. Assignee Suzhou Xinen Pharmaceutical Technology Co., Ltd., Peop. Rep. China. CN 107141298. (2017).

Ticagrelor - Synthetic Route 7

Synthetic reference

Shatru, Ajat; Saini, Dharamvir; Sharma, Abhishek; Bhaskar, P. Muni; Srivastava, Alka; Vir, Dharam; Agarwal, Ashutosh. A process for the preparation of ticagrelor. IN 2014DE00882. (2016).

Ticagrelor - Synthetic Route 8

Synthetic reference

Guile, Simon; Hardern, David; Ingall, Anthony; Springthorpe, Brian; Willis, Paul. Novel triazolo[4,5-d]pyrimidine compounds. Assignee AstraZeneca UK Limited, UK; AstraZeneca AB. WO 2000034283. (2000).

Ticagrelor - Synthetic Route 9

Synthetic reference

Ticagrelor - Synthetic Route 10