635705-72-5Relevant articles and documents
Chain hydrocarbon substituted isoindoline -1, 3 - diketone PDE4 inhibitor and medicinal use thereof
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, (2021/10/27)
The invention relates to a compound shown I and a racemate thereof. A stereoisomer, a tautomer, an isotope label, a solvate, a polymorph, an ester, a prodrug or a pharmaceutically acceptable salt thereof, and a preparation method thereof, and a medical use thereof, the structure of said formula I being as follows.
Asymmetric Synthesis of β-Aryl β-Imido Sulfones Using Rhodium Catalysts with Chiral Diene Ligands: Synthesis of Apremilast
Syu, Jin-Fong,Gopula, Balraj,Jian, Jia-Hong,Li, Wei-Sian,Kuo, Ting-Shen,Wu, Ping-Yu,Henschke, Julian P.,Hsieh, Meng-Chi,Tsai, Ming-Kang,Wu, Hsyueh-Liang
, p. 4614 - 4618 (2019/06/27)
A chiral rhodium(I)-diene catalyst enabled the one-step synthesis of β-aryl β-imido sulfones under mild reaction conditions. By selection of the chiral diene ligand L1a or L2, each enantiomer of the chiral β-aryl β-imido sulfone target can be accessed with high stereoselectivity. Demonstration of the scope of the reaction, which includes the synthesis of an N-protected chiral β-amino β-phenyl sulfone, culminated with the efficient synthesis of the heteroatom-rich active pharmaceutical ingredient apremilast.
Synthesis and refining method of apremilast
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Paragraph 0023, (2017/08/29)
The invention relates to the field of chemical synthesis, in particular to a novel method for synthesizing and refining apremilast. A new starting raw material is introduced; in a preparation process, by selection of the type and the proportion of a specific solvent and control over reaction conditions, the product yield is high, and particle size of a refined product is qualified; no secondary smashing treatment is needed, and the optical purity is improved; therefore, the requirement on experimental equipment and the cost are reduced, the toxicity is reduced, and occurrence of adverse events is avoided.
