1206630-22-9Relevant articles and documents
Synthesis method of (E)-methyl ester 3-(3,5-difluoro-4-formyl phenyl)acrylic acid
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Paragraph 0052-0054, (2021/07/14)
The invention provides a synthesis method of (E)-methyl ester 3-(3,5-difluoro-4-formyl phenyl)acrylic acid, and relates to the field of organic synthesis. The method comprises the following steps: (1) aldehyde group protection: reacting a compound 1, ammonium chloride and alcohol to obtain a compound 2, wherein the alcohol is selected from monohydric alcohol or dihydric alcohol; (2) introducing formyl: reacting the compound 2 serving as a raw material with an organic metal reagent in an organic solvent, and then adding N,N-dimethylformamide for reaction to obtain a compound 3; (3) Wittig-Horner reaction: adding alkali and a compound containing a phosphonate group into the compound 3, and reacting to obtain a compound 4; and (4) deprotection reaction: adding a compound containing a sulfonic acid group and water into the compound 4, and reacting to obtain the product. The synthesis method does not use a noble metal catalyst, so that the cost is obviously reduced; and the product prepared by the synthesis method is high in yield, high in purity, environment-friendly, high in safety and suitable for industrial production, and has a good application prospect.
SOLID FORMS OF 3-((1R,3R)-1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)AZETIDIN-3-YL)AMINO)PHENYL)-3-METHYL-1,3,4,9-TETRAHYDRO-2H-PYRIDO[3,4-B]INDOL-2-YL)-2,2-DIFLUOROPROPAN-1-OL AND PROCESSES FOR PREPARING FUSED TRICYCLIC COMPOUNDS COMPRISING A SUBSTITUTED PHENYL OR PYRIDINYL MOIETY, INCLUDING METHODS OF THEIR USE
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Paragraph 0411; 0548-0549, (2020/01/11)
Provided herein are solid forms, salts such as compound B, and formulations of 3-((lR,3R)-l-(2,6-difluoro-4-((l-(3-fluoropropyl) azetidin-3-yl)amino)phenyl)-3-methyl-l,3,4,9-tetrahydro-2H- pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-l-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
INHIBITORS OF JANUS KINASES
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Page/Page column 56-57, (2010/04/03)
The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.