Scinopharm Taiwan, Ltd.

Tsung-Cheng Hu

Wen-Wei Lin

YuanChang Huang

Piin-Jye Harn

Yuan-Chang Huang

Kuan-Hsun Huang

Li-Ting Wang

Shu-Ping Chen

Ming-Chih Wu

Wei-Shuo Lo

Kuan-Hsun Wang

Yung-Hung Chang

Yu-Sheng Lin

Hsiao-Ping Fang

Hsiao-ping Fang

Inze Lin

Chia-Lin Charlene Shieh

Hong-Tsung Huang

Kuan Hsun Wang

Chung-Yang Huang

Hung-Tsung Huang

Provided herein are improved processes and methods for preparing osimertinib or a salt thereof, in particular osimertinib mesylate. The improved process removes the necessity of isolating the unstable aniline intermediate of formula (III) and enables the direct coupling to form the amide product of formula (II): The present invention is suitable for a large-scale production, avoiding the isolation of unstable intermediate, thereby providing osimertinib or a mesylate salt thereof in both high yields and high purity.

Process for preparing osimertinib or a salt thereof

In certain aspects, the invention provides crystalline forms of ivacaftor N-(2,4-di-tert-butyl-phenyl-5-hydroxy-phenyl)-1,4-dihydro-4-oxoquinoline-3-carboxamide. In related aspects, the invention provides a process for preparing any one of crystalline forms S2, S3, S4 and S5 of ivacaftor. The process includes: forming a solution including crude ivacaftor and a solvent; adding an anti-solvent to the solution to form slurry including a precipitate; isolating the precipitate; and drying the precipitate to provide crystalline form S2, S3, S4, or S5 of ivacaftor.

Crystalline form of ivacaftor and a process for preparing the same

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

Crystalline form S1 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 10.7&#xb1;0.2, 16.2&#xb1;0.2, 19.9&#xb1;0.2, 22.1&#xb1;0.2, 24.7&#xb1;0.2, and 25.9&#xb1;0.2 degrees two-theta, crystalline form S2 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 16.4&#xb1;0.2, 24.9&#xb1;0.2, and 26.2&#xb1;0.2 degrees two-theta, and processes of making thereof are provided.

Crystal forms of lifitegrast

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

Crystalline forms of olaparib and manufacturing processes therefor

The present invention provides novel crystalline forms of apremilast hemitoluene solvate, apremilast hydrate, and apremilast anhydrate and an amorphous form of apremilast, and processes for the preparation of these forms.

Forms of apremilast and the process of making the same

A process of making entecavir comprising converting a compound of formula (M5) to entecavir,wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.

Process for preparing entecavir and its intermediates

Novel crystalline forms of topotecan hydrochloride and processes of making the same are disclosed.

Crystalline forms of topotecan hydrochloride and processes for making the same

A process of making topotecan or a pharmaceutically acceptable salt thereof comprising reacting an iminium salt with 10-hydroxy-camptothecin.

Process for making topotecan

A new compound of formula (IV) R represents a protecting group which is removable by hydrogenation, and use thereof as an intermediate for preparing paliperidone.

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Tainan, Taiwan

Tsung-Cheng Hu