- Methods for preparation of apremilast
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The present invention discloses a method for preparation of Apremilast. β-phthalimino vinylsulfones are reacted through the asymmetric addition reaction to form an addition product, and the drug of Apremilast can be obtained from the addition product through simple reactions. The method is a process for synthesizing Apremilast in a more efficient way.
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Page/Page column 20-21
(2021/05/19)
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- Boron Containing PDE4 Inhibitors
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The present invention relates to boron containing compounds of Formula (I) [in-line-formulae]X—Y—Z?? Formula (I)[/in-line-formulae] that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
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Paragraph 0601-0602
(2020/04/29)
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- Asymmetric Synthesis of β-Aryl β-Imido Sulfones Using Rhodium Catalysts with Chiral Diene Ligands: Synthesis of Apremilast
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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.
- 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
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supporting information
p. 4614 - 4618
(2019/06/27)
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- Synthesis of 2,2-Dimethyl-2H-thiochromenes, the Sulfur Analogs of Precocenes
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A new general synthesis of 2,2-dimethyl-2H-thiochromenes in good yield consists of the Michael addition of thiophenols to 3-methyl-2-butenoic acid, intramolecular cyclocondensation of the resultant 3-methyl-3-phenylthiobutanoic acids, reduction of the 2,2-dimethyl-4-oxothiochromenes thus obtained with sodium borohydride, and acid-catalyzed dehydration of the resultant 4-hydroxy-2,2-dimethylthiochromans.
- Tercio, J.,Ferreira, B.,Catani, V.,Comasseto, J. V.
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p. 149 - 153
(2007/10/02)
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