945950-37-8Relevant articles and documents
PROCESS AND INTERMEDIATES FOR PREPARING A JAK INHIBITOR
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, (2022/03/04)
The present invention is related to processes for preparing ruxolitinib, or a salt thereof, and related synthetic intermediates related thereto.
PROCESS AND INTERMEDIATES FOR PREPARING A JAK1 INHIBITOR
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, (2022/03/02)
The present invention is related to processes for preparing itacitinib, or a salt thereof, and related synthetic intermediates related thereto.
Preparation method of key intermediate of JAK inhibitor
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Paragraph 0043; 0048; 0049; 0050; 0055-0057; 0062; 0063, (2021/09/04)
The invention discloses a preparation method of a key intermediate of a JAK inhibitor. The preparation method comprises the following steps: step a, protecting an amino group of a raw material 4-chloro-7H-pyrrole-[2.3-d]-pyrimidine to synthesize 4-chloro-
Method for catalytically synthesizing 7-denitrified purine compound by using iron coordination compound
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Paragraph 0073-0077, (2021/10/27)
The invention relates to a method for catalytically synthesizing a 7-denitrogenated purine compound by using an iron coordination compound. The method comprises the following steps: in the presence of an alkali, taking 7-denitrogenated purine and halogenated hydrocarbon as raw materials, taking an iron coordination compound containing an ortho-carborane benzoxazole structure as a catalyst, and reacting at room temperature to obtain the 6-substituted 7-denitrogenated purine compound. Compared with the prior art, the method has the advantages that the iron coordination compound containing the ortho-carborane benzoxazole structure is utilized to catalytically synthesize the 6-substituted 7-deazapurine compound, so that the compound is prepared by a one-pot method at room temperature, the use equivalent of the catalyst is low, the reaction condition is mild, the raw materials are cheap and easy to obtain, the substrate universality is high, and the yield is high.
Synthesis method of 4-methyl-7H-pyrrolo[2,3-d]pyrimidine
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Paragraph 0033; 0036-0039; 0042-0043; 0046-0047; 0050-0051, (2021/04/21)
The invention provides a synthesis method of 4-methyl-7H-pyrrolo[2,3-d]pyrimidine, wherein the comprises the following steps: (a) reacting a substance represented by a formula (I) with a methyl Grignard reagent under the action of a catalyst to obtain a compound represented by a formula (II); and (b) carrying out dechlorination reaction on the compound represented by the formula (II) under the action of a reducing agent to obtain a compound represented by a formula (III). According to the preparation method, starting raw materials, process routes and post-treatment processes are different, the raw materials are simple and easy to obtain, the cost is low, and the preparation method is suitable for laboratory small-scale preparation and industrial production.
NOVEL 6-SUBSTITUTED 7-DEAZAPURINES AND CORRESPONDING NUCLEOSIDES AS MEDICAMENTS
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Page/Page column 25-26; 28; 48, (2021/08/27)
The present invention relates to the synthesis of 6-substituted 7-deazapurines and their corresponding nucleosides by coupling aryl or alkyl Grignard reagents with halogenated purine nucleosides in the presence of iron or an iron/copper mixture such as Fe(acac)3/Cul. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections.
IRREVERSIBLE INHIBITORS OF MENIN-MLL INTERACTION
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Paragraph 00602, (2020/07/21)
Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.
SYNTHESIS PROCESS OF RUXOLITINIB
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Paragraph 0241-0243, (2019/02/05)
The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.
Iron/Copper Co-Catalyzed Cross-Coupling Reaction for the Synthesis of 6-Substituted 7-Deazapurines and the Corresponding Nucleosides
Daelemans, Dirk,Herdewijn, Piet,Li, Qingfeng,Persoons, Leentje
, (2020/01/03)
An efficient access to 6-substituted 7-deazapurine and the corresponding nucleosides by coupling aryl or alkyl Grignard reagents and halogenated purine nucleosides in the presence of Fe(acac)3/CuI is described. A series of 6-substituted 7-deazapurines and the corresponding nucleosides were obtained in medium to good yields. For the synthesis of modified nucleosides that will be the subject of biological testing, we propose to use iron-catalyzed instead of palladium-catalyzed reaction. The synthesized compounds were tested for their antiproliferative activity. The cytotoxicity study of compounds 11a-q shows that by modifying the 6-position of 7-deazapurine ribonucleosides, the compounds may become selective for certain cancer cell lines.
LIM KINASE INHIBITORS, PHARMACEUTICAL COMPOSITION AND METHOD OF USE IN LIMK-MEDIATED DISEASES
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Page/Page column 43, (2018/04/20)
The present invention relates to LIM Kinase inhibitors of Formula (I) and pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, R3, R4, X1, X2, X3, Y1, Y2 and Z are as defined in the claims, and their use for the treatment and/or prevention of LIMK-mediated diseases.
