608141-42-0Relevant articles and documents
CRYSTAL FORMS OF THIOPHENE DERIVATIVES
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Paragraph 0271, (2021/05/14)
Disclosed is crystal form I of compound (S)—N-[5-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4,6-dioxo-5,6-dihydro-4H-thieno[3,4-c]pyrrole-1-yl]acetamide.
Synthesis method of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl) ethylamine
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Paragraph 0164-0176, (2021/01/29)
The invention relates to a synthetic method of (S)-1-(3-ethoxy-4-methoxy phenyl)-2-(methylsulfonyl) ethylamine. The method comprises the following steps: mixing 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl) vinylamine, a chiral catalyst, an acid and a solvent, and performing reacting; the structural formula of the chiral catalyst is shown as a formula (I), wherein R is selected from a hydrogen atom, an alkyl group, an aromatic ring, an alkoxy group, a halogen atom, an amino group, a cyano group, a hydroxyl group, a trifluoromethyl group, a nitro group, an ester group or an amido group. (S)-1-(3-ethoxy-4-methoxy phenyl)-2-(methylsulfonyl) ethylamine with high chiral purity can be generated in one step, meanwhile, the product is easy to separate and purify, and the yield is high. In addition, the method is mild in reaction condition, stable in process, simple and safe in reaction operation, low in production cost, simple and feasible in three-waste treatment, environment-friendly, easily available in raw materials, low in production cost and suitable for industrial production.
Preparation method of PDE-4 inhibitor intermediate
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, (2020/11/26)
The invention provides a preparation method of a PDE-4 inhibitor intermediate, and belongs to the field of medicinal chemistry. The method comprises the following steps: halogenating a compound 01 toobtain a compound 02, performing hydroxylation to obtain a brand-new compound 03, reacting the compound 03 with a sulfonylation reagent to obtain a compound 04, reducing the compound 04 with a transition metal catalyst to obtain a compound 05, and reacting the compound 05 under the action of a methanesulfinic acid reagent to generate a target compound 06. The method is mild in reaction condition,simple in technological operation, high in yield, high in product purity, good in selectivity and beneficial to industrial production.