Tipiracil HCl synthetic routes

CAT#: 206037 | Name: Tipiracil HCl | CAS# 183204-74-2

Purchases for research

Description:

Tipiralacil, also known as TPI, is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials. TAS-102 consists of the cytotoxin Trifluridine and the thymidine phosphorylase inhibitor (TPI) tipiracil. Trifluridine is incorporated into DNA during DNA synthesis and inhibits tumor cell growth. Tipiracil protects trifluridine from being broken down when taken orally. TAS-102 was approved in Japan in 2015.

Synthetic Routes

Tipiracil HCl - Synthetic Route 1

Tipiracil HCl - Synthetic Route 1

Synthetic Description

Ref: Maheta, Abhay Subodhbhai; Kaneria, Ankur Amrutlal; Bhesaniya, Kapil Dhanjibhai; Savaliya, Bhavesh Laljibhai; Koilpillai, Joseph Prabahar; Agarwal, Virendra Kumar; Chavan, Rahul Baburao; Arabiani, Mohsin Razakbhai; Hedapara, Kalpesh Ratilal; Katariya, Lalit Keshav; Patel, Vijay Premajibhai; Thummar, Mahesh Kurajibhai; Bhalodiya, Rahul Harsukhlal. Process for the preparation of tipiracil hydrochloride (Assignee Amneal Pharmaceuticals Company GmbH, Switz.). WO 2019002407 (2019).

Tipiracil HCl - Synthetic Route 2

Tipiracil HCl - Synthetic Route 2

Synthetic Description

Gao, Dalong; Yang, Qingkun; Zhou, Xuewen; Li, Baoyong; Wu, Ke; Zhang, Zhaozhen; Dong, Tinghua; Yang, Boyong (Assignee Qilu Tianhe Pharmaceutical Co., Ltd., Peop. Rep. China). Preparation method of tipiracil. CN 106749194 (2017)

Tipiracil HCl - Synthetic Route 3

Tipiracil HCl - Synthetic Route 3

Synthetic Description

Reference: Wang, Shujuan; Xu, Hao; Kang, Wei Assignee Sinopharm A-Think Pharmaceutical Co., Ltd., Peop. Rep. China. Synthesis method of tipiracil hydrochloride as antitumor drug and its intermediate 6-chloromethyl uracil. CN 106892902. (2017).

Synthetic Reference

Wang, Shujuan; Xu, Hao; Kang, Wei Assignee Sinopharm A-Think Pharmaceutical Co., Ltd., Peop. Rep. China. Synthesis method of tipiracil hydrochloride as antitumor drug and its intermediate 6-chloromethyl uracil. CN 106892902. (2017).

Tipiracil HCl - Synthetic Route 4

Tipiracil HCl - Synthetic Route 4

Synthetic Reference

Sun, Ping; Li, Sai; Du, Zuyin; Zhao, Junjun; Li, Xiaobi. Process for the preparation of 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidinedione hydrochloride. Assignee Jiangsu Hansoh Pharmaceutical Co., Ltd., Peop. Rep. China; Jiangsu Hansoh Pharmaceutical Group, Lianyungang Grand Champ Medicine Co., Ltd. CN 104945384 A (2015)