US 11,702,439 B2
Method for preparing trifluridine
Lin Liu, Jiangsu (CN); Rui Zhao, Jiangsu (CN); Guangming Sang, Jiangsu (CN); Xingjian Zhou, Jiangsu (CN); Xiaopeng Guo, Jiangsu (CN); Aiming Zhang, Jiangsu (CN); Gang Wu, Jiangsu (CN); Chunguang Xia, Jiangsu (CN); and Xiquan Zhang, Jiangsu (CN)
Assigned to CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., Jiangsu (CN)
Appl. No. 17/262,186
Filed by CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., Jiangsu (CN)
PCT Filed Jul. 24, 2019, PCT No. PCT/CN2019/097439
§ 371(c)(1), (2) Date Jan. 21, 2021,
PCT Pub. No. WO2020/020208, PCT Pub. Date Jan. 30, 2020.
Claims priority of application No. 201810817373.6 (CN), filed on Jul. 24, 2018.
Prior Publication US 2021/0292356 A1, Sep. 23, 2021
Int. Cl. C07H 19/06 (2006.01)
CPC C07H 19/06 (2013.01) 19 Claims
 
1. A method for preparing a compound of formula II, wherein a compound of formula III and a compound of formula IV are reacted in a first solvent in the presence of an acid to obtain the compound of formula II,

OG Complex Work Unit Chemistry
wherein, X is a halogen atom;
R1 and R2 are each independently hydrogen, methyl or halogen atoms;
R3 and R4 are hydroxyl protecting groups; and
the acid is one or a mixture of two or more of HCl, formic acid, acetic acid, or acetic anhydride.