- Method for preparing bosutinib intermediate
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The invention provides a method for preparing a bosutinib intermediate. The method comprises the following steps: A, adding SM-1, 1-bromo-3-chloropropane and an acid-binding agent into a reaction solvent, controlling the temperature until the reaction is
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Paragraph 0079-0080
(2020/09/20)
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- HISTONE METHYLTRANSFERASE INHIBITORS
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The present disclosure provides certain angular tricyclic compounds that are histone methyltransi erases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinpathies (e.g., beta- thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
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Page/Page column 106
(2018/07/29)
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- Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma
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The BTK and JAK3 receptor tyrosine kinases are two validated and therapeutically amenable targets in the treatment of B-cell lymphomas. Here we report the identification of several classes of pyrimidine derivatives as potent BTK and JAK3 dual inhibitors.
- Ge, Yang,Wang, Changyuan,Song, Shijie,Huang, Jiaxin,Liu, Zhihao,Li, Yongming,Meng, Qiang,Zhang, Jianbin,Yao, Jihong,Liu, Kexin,Ma, Xiaodong,Sun, Xiuli
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p. 1847 - 1857
(2017/12/04)
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- PYRIMIDINE-2,4-DIAMINE DERIVATIVES AND THEIR USE AS JAK2 KINASE INHIBITORS
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Pyrimidine-2,4-diamines derivatives having activity as JAK2 kinase inhibitors are disclosed, as well as pharmaceutical compositions and methods for using the same in the treatment of cancer and other JAK2 kinase-associated conditions.
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Page/Page column 19
(2008/12/08)
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- Process for preparation of 4-amino-3-quinolinecarbonitriles
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This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.
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Page/Page column 7
(2010/02/10)
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- PHOTOINDUCED INTRAMOLECULAR SUBSTITUTION-III PHOTOCYCLIZATION OF ω-ANILINOALKYL m-NITROPHENYL ETHERS
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Irradiation of 1-(m-nitrophenoxy)-ω-anilinoalkanes, m-O2NC6H4O(CH2)nNHPh (n = 2 and 3) and their 1-(2-methoxy-5-nitrophenoxy) analogs induced intramolecular cyclization in which a hydrogen or methoxyl
- Mutai, Kiyoshi,Kobayashi, Keiji,Yokoyama, Kenji
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p. 1755 - 1760
(2007/10/02)
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