Scinopharm Taiwan, Ltd.

Yung-Hung Chang

Tsung-Yu Hsiao

Tsung-Cheng Hu

Yuan-Xiu Liao

Wen-Wei Lin

Yuan-Chang Huang

Kuan-Hsun Wang

Hsin-Chang Tseng

The present invention provides improved processes for the preparation of elagolix and intermediates thereof. The intermediate of formula VII is achieved by a coupling reaction of a compound of formula V and a N-benzylidene protected compound of formula IV: The present invention is suitable for a large-scale production, avoiding the use of potential genotoxic substances and can be performed under mild conditions.

Process for preparing elagolix sodium and intermediates thereof

In certain aspects, the invention provides a novel crystalline form of olaparib (4-[(3-[(4-cyclopropylcarbonyl)piperazin-4-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one). In related aspects, the invention provides a processe for preparing the novel crystalline form of olaparib. The process includes forming a solution comprising crude olaparib and an organic solvent; adding the solution to an anti-solvent to form a slurry comprising a precipitate; isolating the precipitate; and drying the precipitate to obtain a crystalline form III of olaparib.

Crystalline form of olaparib and a process for preparing the same

Provided herein are novel processes and methods for making 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one (Olaparib) and intermediates thereof. Olaparib is a poly ADP ribose polymerase (PARP) inhibitor useful in the treatment of cancers. Benefits of the present disclosure include the use of less toxic compounds and improved yields.

Processes for preparing olaparib

Growing community of inventors

Tainan, Taiwan

Yung-Hung Chang