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Olaparib

CAT#: H200422

CAS#: 763113-22-0

Description: Olaparib, also known as AZD-2281 or KU-59436 , is a small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.

Synthetic Routes

Olaparib - Synthetic Route 1

Synthetic reference

Zmuda, Filip; Malviya, Gaurav; Blair, Adele; Boyd, Marie; Chalmers, Anthony J.; Sutherland, Andrew; Pimlott, Sally L. Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo. Journal of Medicinal Chemistry. Volume 58. Issue 21. Pages 8683-8693. Journal; Online Computer File. (2015).

Olaparib - Synthetic Route 2

Synthetic reference

Lindhardt, Anders T.; Simonssen, Roger; Taaning, Rolf H.; Gogsig, Thomas M.; Nilsson, Goeran N.; Stenhagen, Gunnar; Elmore, Charles S.; Skrydstrup, Troels. 14Carbon monoxide made simple - novel approach to the generation, utilization, and scrubbing of 14carbon monoxide. Journal of Labelled Compounds and Radiopharmaceuticals. Volume 55. Issue 11. Pages 411-418. Journal; Online Computer File. (2012).

Olaparib - Synthetic Route 3

Synthetic reference

Rao, Mahender; Velisoju, Mahendar; Anegondi, Shreenivasa Prasad; Joshi, Yogesh Vasant; Panwar, Amit. Process for the preparation of olaparib and polymorphs thereof. Assignee Alembic Pharmaceuticals Limited, India. IN 201621015481. (2017).

Olaparib - Synthetic Route 4

Synthetic reference

Liu, Zhenteng; Xu, Shuzhou; Han, Yunlong; Chai, Qian. Method for refining Olaparib. Assignee Shandong Yuxin Pharmaceutical Co., Ltd., Peop. Rep. China. CN 108586355. (2018).

Olaparib - Synthetic Route 5

Synthetic reference

Qiao, Hongwei; Bian, Weiguang; Li, Qiaoying. Method for synthesizing olaparib containing phthalhydrazide. Assignee Beijing Yaocheng Huiren Technology Co., Ltd., Peop. Rep. China. CN 108129397. (2018).

Olaparib - Synthetic Route 6

Synthetic reference

Liu, Zhenteng; Sun, Yiwei; Li, Hua; Gong, Wenju; Wang, Libiao. Preparation of Olaparib. Assignee Shandong Yuxin Pharmaceutical Co., Ltd., Peop. Rep. China. CN 107325055. (2017).

Olaparib - Synthetic Route 7

Synthetic reference

Wang, Liqiang; Qiu, Fei; Yue, Haitao. Preparation method of olaparib and its analog. Assignee Guangzhou Youmijian Pharmaceutical Technology Co., Ltd., Peop. Rep. China. CN 105085407. (2015).