Tapentadol

CAT#: H318791

CAS#: 175591-23-8


Description: Tapentadol has been discontinued (DEA controlled substance). Tapentadol is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Tapentadol general potency is somewhere between that of tramadol and morphine, with an analgesic efficacy comparable to that of oxycodone despite a lower incidence of side effects. It is generally regarded as a weak-moderate strength opioid.

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Synthetic Routes

Tapentadol - Synthetic Route 1

Tapentadol route01

Synthetic reference

Khunt, Mayur Devjibhai; Bondge, Sandipan Prabhurao; Patil, Nilesh Sudhir; Pagire, Haushabhau Shivaji; Pradhan, Nitin Sharadchandra. Preparation of highly pure tapentadol or a pharmaceutically acceptable salt. Assignee Actavis Group PTC EHF, Iceland. WO 2011128784. (2011).

Tapentadol - Synthetic Route 2

Tapentadol route02

Synthetic reference

Bhirud, Shekhar Bhaskar; Johar, Perminder Singh; Sharma, Ekta; Jamshad, Danish; Prajapaty, Ramkaran. Process for the preparation of 1-phenyl-3-dimethylaminopropane derivatives. Assignee Ind-Swift Laboratories Limited, India. WO 2011092719. (2011).

Tapentadol - Synthetic Route 3

Tapentadol route03

Synthetic reference

Motta, Giuseppe; Vergani, Domenico; Bertolini, Giorgio; Landoni, Nicola. Process for preparation of tapentadol and intermediates thereof. Assignee Archimica Srl, Italy. WO 2012001571. (2012).

Tapentadol - Synthetic Route 4

Tapentadol route04

Synthetic reference

Rajan, Srinivasan Thirumalai; Rao, Gogulapati Venkata Panakala. Process for the preparation of 3-aryl-2-methyl-propanamine derivatives and polymorphs thereof. Assignee MSN Laboratories Limited, India. IN 2012CH00097. (2013).

Tapentadol - Synthetic Route 5

Tapentadol route05

Synthetic reference

Vlasakova, Ruzena; Hajicek, Josef. Process for preparing (2R,3R)-N,N-dimethyl-3-(hydroxyphenyl)-2-methylpentylamine (tapentadol). Assignee Zentiva, K.S., Czech Rep. CZ 302992. (2012).

Tapentadol - Synthetic Route 6

Tapentadol route06

Synthetic reference

Franklin, Richard; Golding, Bernard; Swift, Karl; Tyson, Robert. Preparation of opioids prodrugs for treating pain. Assignee Shire LLC, USA. WO 2011083304. (2011).

Tapentadol - Synthetic Route 7

Tapentadol route07

Synthetic reference

Sun, Zhankui; Liu, Yongjian; Li, Haihong; Wang, Mingjun; Zhang, Nianyu; Wang, Zhisheng. A process for preparing tapentadol and intermediates thereof. Assignee Topharman Shanghai Co., Ltd., Peop. Rep. China; Topharman Shandong Co., Ltd. WO 2011026314. (2011).

Tapentadol - Synthetic Route 8

Tapentadol route08

Synthetic reference

Liao, Subo; McClurg, Joseph; Trawick, Bobby. Process for preparing substituted phenylalkanes. Assignee Mallinckrodt LLC, USA. WO 2016007823. (2016).

Tapentadol - Synthetic Route 9

Tapentadol route09

Synthetic reference

Kljajic, Alen; Simoncic, Ana Bergant; Pecavar, Anica; Zupet, Rok; Smirnova, Elena. Tapentadol maleate and crystalline forms thereof. Assignee Farma GRS, D. O. O., Slovenia. WO 2014108514. (2014).

Tapentadol - Synthetic Route 10

Tapentadol route010

Synthetic reference

Rajadhyaksha, Mangesh Narayan; Nair, Ranjeet; Deshmukh, Sandip Kacharu; Khabale, Somnath Ambadas; Panandikar, Aditi Milindi. Process for the preparation of tapentadol. Assignee Indoco Remedies Limited, India. IN 2010MU02303. (2013).