- AZETIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
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The present invention relates to an azetidine derivative for use as a Janus kinase (JAK) inhibitor, a drug composition comprising same, a preparation method therefor, and a use thereof in the treatment of JAK-related diseases comprising, for example, infl
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- Preparation method for Baricitinib intermediate
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The invention belongs to the field of pharmaceutical and chemical industry, and particularly relates to a preparation method for a Baricitinib intermediate. The preparation method is characterized in that a key intermediate 2-[1-ethyl sulfonyl-3-[4-(4,4,5,5- tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-parazole-1-ethyl] azacyclobutyl-3-yl) acetonitrile is prepared through reaction of a 4-parazole boride and 2-[1-(ethyl sulfonyl-3-azacyclobutaneylidene) acetonitrile, and nitrogen on a pyrazolone ring of 4- parazole boride does not need to be protected, so that a follow-up step of removing a corresponding a protective group is avoided, and therefore, the whole reaction route is short, raw materials are obtained easier, the production cost is low, and the preparation method is especially suitable for industrial production.
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- AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
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The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
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Page/Page column 58-60
(2009/09/28)
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