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Alectinib synthetic routes

Alectinib - Synthetic Route

CAT#: 205799 | Name: Alectinib | CAS# 1256580-46-7

Purchases for research

Description:

Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Alectinib was approved in Dec. 2015.

Synthetic Routes

Alectinib - Synthetic Route 1

Alectinib - Synthetic Route 1

Synthetic Description

Reference: Xu, Xuenong. Alectinib preparation method. CN 104402862. (Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China)

Synthetic Reference

Xu, Xuenong. Alectinib preparation method. CN 104402862. (Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China)

Alectinib - Synthetic Route 2

Alectinib - Synthetic Route 2

Synthetic Description

Reference: Liu, Ye; Xiong, Yuanqiang. Process for the preparation of alectinib from 6-bromo-3,4-dihydro-2(1H)-naphthalenone. CN 105777710. (Assignee Hunan Ouya Biological Co., Ltd., Peop. Rep. China)

Synthetic Reference

Liu, Ye; Xiong, Yuanqiang. Process for the preparation of alectinib from 6-bromo-3,4-dihydro-2(1H)-naphthalenone. CN 105777710. (Assignee Hunan Ouya Biological Co., Ltd., Peop. Rep. China)

Alectinib - Synthetic Route 3

Alectinib - Synthetic Route 3

Synthetic Description

Reference: Chen, Peng; Zhao, Guolei. Process for preparation of Alectinib. CN 106518842. (Assignee Beijing Wanquan Dezhong Pharmaceutical Biotechnology Co., Ltd., Peop. Rep. China)

Synthetic Reference

Chen, Peng; Zhao, Guolei. Process for preparation of Alectinib. CN 106518842. (Assignee Beijing Wanquan Dezhong Pharmaceutical Biotechnology Co., Ltd., Peop. Rep. China)

Alectinib - Synthetic Route 4

Alectinib - Synthetic Route 4

Synthetic Description

Reference: Chen, Jian; Huang, Wei; Zhong, Yunjian. Preparation method of alectinib from 2-(4-bromo-3-hydroxyphenyl)acetate. CN 106995433. (Assignee Hunan Boaode Biopharmaceutical Technology Development Co., Ltd., Peop. Rep. China)

Synthetic Reference

Chen, Jian; Huang, Wei; Zhong, Yunjian. Preparation method of alectinib from 2-(4-bromo-3-hydroxyphenyl)acetate. CN 106995433. (Assignee Hunan Boaode Biopharmaceutical Technology Development Co., Ltd., Peop. Rep. China)

Alectinib - Synthetic Route 5

Alectinib - Synthetic Route 5

Synthetic Description

Reference: Ning, Ting; Tong, Ming; Li, Tao. Preparation method of alectinib. CN 107033125. (Assignee Hunan Boaode Biopharmaceutical Technology Development Co., Ltd., Peop. Rep. China)

Synthetic Reference

Ning, Ting; Tong, Ming; Li, Tao. Preparation method of alectinib. CN 107033125. (Assignee Hunan Boaode Biopharmaceutical Technology Development Co., Ltd., Peop. Rep. China)

Alectinib - Synthetic Route 6

Alectinib - Synthetic Route 6

Synthetic Description

Reference: Lin, Kaichao; Huang, Wei; Zhang, Jianguo. Method for preparing alectinib. CN 107129488. (Assignee Hunan Boaode Biopharmaceutical Technology Development Co., Ltd., Peop. Rep. China)

Synthetic Reference

Lin, Kaichao; Huang, Wei; Zhang, Jianguo. Method for preparing alectinib. CN 107129488. (Assignee Hunan Boaode Biopharmaceutical Technology Development Co., Ltd., Peop. Rep. China)

Alectinib - Synthetic Route 7

Alectinib - Synthetic Route 7

Synthetic Description

Reference: Dong, Dandan. Method for preparation of Alectinib. CN 107987056.

Synthetic Reference

Dong, Dandan. Method for preparation of Alectinib. CN 107987056.

Alectinib - Synthetic Route 8

Alectinib - Synthetic Route 8

Synthetic Description

Reference: Furumoto, Kentaro; Shiraki, Koji; Hirayama, Tomoaki. Composition containing tetracyclic compound and dissolution aid. WO 2012023597. (Assignee Chugai Seiyaku Kabushiki Kaisha, Japan)

Synthetic Reference

Furumoto, Kentaro; Shiraki, Koji; Hirayama, Tomoaki. Composition containing tetracyclic compound and dissolution aid. WO 2012023597. (Assignee Chugai Seiyaku Kabushiki Kaisha, Japan)

Alectinib - Synthetic Route 9

Alectinib - Synthetic Route 9

Synthetic Description

Reference: Xu, Xuenong. Alectinib preparation method. WO 2016074532. (Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China; Zheren Pharmaceutical Nanjing Co., Ltd.)

Synthetic Reference

Xu, Xuenong. Alectinib preparation method. WO 2016074532. (Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China; Zheren Pharmaceutical Nanjing Co., Ltd.)

Alectinib - Synthetic Route 10

Alectinib - Synthetic Route 10

Synthetic Reference

Kinoshita, Kazutomo; Asoh, Kohsuke; Furuichi, Noriyuki; Ito, Toshiya; Kawada, Hatsuo; Hara, Sousuke; Ohwada, Jun; Miyagi, Takuho; Kobayashi, Takamitsu; Takanashi, Kenji; Tsukaguchi, Toshiyuki; Sakamoto, Hiroshi; Tsukuda, Takuo; Oikawa, Nobuhiro. Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802). Bioorganic & Medicinal Chemistry. Volume 20. Issue 3. Pages 1271-1280. 2012.