Tolvaptan

CAT#: H317142

CAS#: 150683-30-0

Description: Tolvaptan is a selective, competitive vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH).

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Synthetic Routes

Tolvaptan - Synthetic Route 1

Tolvaptan route01

Synthetic reference

Cordero-Vargas, Alejandro; Quiclet-Sire, Beatrice; Zard, Samir Z. A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan. Bioorganic & Medicinal Chemistry. Volume 14. Issue 18. Pages 6165-6173. 2006.

Tolvaptan - Synthetic Route 2

Tolvaptan route02

Synthetic reference

Torisawa, Yasuhiro; Abe, Kaoru; Muguruma, Yasuaki; Fujita, Shigekazu; Ogawa, Hidenori; Utsumi, Naoto; Miyake, Masahiro. Process for preparation of benzoylaminobenzoylbenzazepinones by reaction of benzazepinones with benzoylaminophenyl halides in the presence of carbonylating agents. Assignee Otsuka Pharmaceutical Co., Ltd., Japan. WO 2007026971. (2007).

Tolvaptan - Synthetic Route 3

Tolvaptan route03

Synthetic reference

Zard, Samir; Cordero Vargas, Alejandro; Sire, Beatrice. Improved process for the preparation of benzazepines and their derivatives. Assignee Centre National de la Recherche Scientifique CNRS, Fr.; Ecole Polytechnique. FR 2867187. (2005).

Tolvaptan - Synthetic Route 4

Tolvaptan route04

Synthetic reference

Gao, Junlong; Li, Peng; Liu, Kai; Guo, Dapeng. Method for preparing high-purity Tolvaptan intermediate. Assignee Jiangsu Hengrui Medicine Co., Ltd., Peop. Rep. China. CN 108503586. (2018).

Tolvaptan - Synthetic Route 5

Tolvaptan route05

Synthetic reference

Han, Shin; Jeon, Seong Hyeon; Lee, Shin Yoon. Improved method for preparing synthetic intermediates for tolvaptan. Assignee Hexa Pharmatec Co., Ltd., S. Korea. JP 2018012690. (2018).

Tolvaptan - Synthetic Route 6

Tolvaptan route06

Synthetic reference

Guo, Xinfu; Wang, Qiang; Liu, Zhaoguo; Wang, Zhipeng. Preparation method of tolvaptan. Assignee Tianjin Taipu Pharmaceutical Co., Ltd., Peop. Rep. China. CN 106883175. (2017).

Tolvaptan - Synthetic Route 7

Tolvaptan route07

Synthetic reference

Lixin, Juanzi; Li, Jianzhi; Ma, Xilai; Chi, Wangzhou; Liu, Hai; Hu, Xuhua; Zheng, Xiaoli; Zhai, Zhijun; Li, Jianxun. Process for the preparation of tolvaptan. Assignee Shanghai Tianci International Pharmaceutical Co., Ltd., Peop. Rep. China. CN 105753735. (2016).

Tolvaptan - Synthetic Route 8

Tolvaptan route08

Synthetic reference

Patel, Dhaval J.; Shah, Tejas C.; Singh, Manoj Kumar. A process for the preparation of tolvaptan. Assignee Cadila Healthcare Limited, India. IN 2012MU01559. (2014).

Tolvaptan - Synthetic Route 9

Tolvaptan route09

Synthetic reference

Sethi, Madhuresh Kumar; Rawat, Vijendrasingh; Thirunavukarasu, Jayaprakash; Yerramala, Raja Krishna; Kumar, Anish. Improved process for the preparation of tolvaptan. Assignee Matrix Laboratories Ltd., India. IN 2011CH01303. (2013).

Tolvaptan - Synthetic Route 10

Tolvaptan route010

Synthetic reference

Chen, Tao; Chen, Hua; Yu, Lingli; Fan, Xiyuan. Method for preparing 2-carboxy-5-(2-methylbenzamido)toluene as Tolvaptan intermediate. Assignee Tianjin Taipu Medicine Science and Technology Development Co., Ltd., Peop. Rep. China. CN 103159641. (2013).