Scinopharm Taiwan, Ltd.

Wei-Shuo Lo

Wen-Wei Lin

YuanChang Huang

Kuan-Hsun Wang

Ying-Tzu Lin

Wan-Yin Cheng

Tsung-Yu Hsiao

Tsung-Cheng Hu

MengFen Ho

Yu-Sheng Lin

Hsiao-ping Fang

HsinChang Tseng

WenShing Tsao

Kuan Hsun Wang

The present invention provides efficient, economical, and improved methods for synthesizing ibrutinib and intermediates thereof. The invention involves a unique biphasic acylation reaction system which advantageously allows for easy separation of ibrutinib from the reaction mixture without additional extraction and wash steps. The isolated ibrutinib formed using the methods described herein can be useful in the preparation of an amorphous form of ibrutinib. In some embodiments, the isolated ibrutinib produced by the processes described herein is a homogenous solution of ibrutinib and DMSO which may be directly used in the formation of the amorphous polymorph. In some embodiments, the isolated ibrutinib is solid ibrutinib. The solid ibrutinib may also be used in the formation of amorphous ibrutinib.

Process for preparing ibrutinib and its intermediates

Crystalline forms of pemetrexed diacid are provided (Forms 1 and 2) which are readily produced for either laboratory-scale or industrial scale. Processes for the preparation of Forms 1 and 2 are also provided.

Crystalline forms of pemetrexed diacid 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

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Tainan, Taiwan

Wei-Shuo Lo