- Synthesis method of 3-aminopyridine formaldehyde
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The invention discloses a synthesis method of 3-aminopyridine formaldehyde, which comprises the following steps of: carrying out a cutius rearrangement reaction on 2-bromonicotinic acid serving as a raw material to obtain tert-butyl (2-bromopyridine-3-yl) carbamate, carrying out a Grignard reaction to obtain tert-butyl (2-formyl pyridine-3-yl) carbamate, and finally carrying out a hydrolysis reaction to obtain 3-aminopyridine formaldehyde. The synthesis method overcomes the defects of expensive raw materials, low yield, use of microwave reaction and other conditions, difficulty in amplification and the like in the existing synthesis process, and has the advantages of simple synthesis route, reasonable process selection, low raw material cost, simple and easily available raw materials, convenience in operation and post-treatment, high total yield, no use of highly toxic reagents, easiness in amplification, and realization of mass production.
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Paragraph 0015; 0018-0019
(2021/02/20)
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- Asymmetric Ruthenium-Catalyzed Hydrogenation of 2,6-Disubstituted 1,5-Naphthyridines: Access to Chiral 1,5-Diaza-cis-Decalins
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The first asymmetric hydrogenation (AH) of 2,6-disubstituted and 2,3,6-trisubstituted 1,5-naphthyridines, catalyzed by chiral cationic ruthenium diamine complexes, has been developed. A wide range of 1,5-naphthyridine derivatives were efficiently hydrogenated to give 1,2,3,4-tetrahydro-1,5-naphthyridines with up to 99% ee and full conversions. This facile and green protocol is applicable to the scaled-up synthesis of optically pure 1,5-diaza-cis-decalins, which have been used as rigid chelating diamine ligands for asymmetric synthesis.
- Zhang, Jianwei,Chen, Fei,He, Yan-Mei,Fan, Qing-Hua
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supporting information
p. 4622 - 4625
(2015/04/14)
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- HETEROCYCLIC COMPOUNDS AND THEIR USES
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Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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Page/Page column 27-28
(2011/07/06)
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