16135-36-7Relevant articles and documents
Facile synthesis of functionalized 4-aminopyridines
Nishiwaki, Nagatoshi,Azuma, Mayumi,Tamura, Mina,Hori, Kazushige,Tohda, Yasuo,Ariga, Masahiro
, p. 2170 - 2171 (2002)
The title compounds are readily available by ring transformation of nitropyrimidinone with active methylene compounds in the presence of ammonium acetate.
High-yield synthesis method of methyl 4-aminonicotinate
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Paragraph 0024; 0030-0033; 0039-0042; 0048-0050, (2021/09/08)
The invention discloses a high-yield synthesis method of methyl 4-aminonicotinate, which comprises the following steps: by taking 3, 4-dipicolinic acid as a raw material, carrying out intramolecular dehydration substitution, ammonia ammonification, improved NBS Hofmann rearrangement and hydrolysis to obtain the methyl 4-aminonicotinate. The synthesis method disclosed by the invention is simpler to operate, mild in reaction condition and higher in total yield, and has an extremely high application value.
Novel Aryl-Modified Benzoylamino-N-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-heteroamides as Potent Inhibitors of Vascular Endothelial Growth Factor Receptors 1 and 2
Ashok, Abhishek,Thanukrishnan, Kannan,Bhojya Naik, Halehatty S.,Maridu, Rajendraswami
, p. 1949 - 1956 (2017/05/29)
Tumor angiogenesis has become an important target for antitumor therapy, with most current therapies aimed at blocking the vascular endothelial growth factor (VEGF) pathway. The VEGF and its receptors have been implicated as key factors in tumor angiogenesis and are major targets in cancer therapy. A series of aryl-modified benzoylamino-N-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-heteroamides were synthesized from 2-amino-5,6-dimethoxy benzimidazole and aryl-substituted benzoylamino hetero acids. The new compounds were tested for inhibition of VEGF receptors I and II (VEGFR-1 and VEGFR-2). Compound 6e displayed VEGFR-2 inhibitory activity with a 50% inhibition concentration value as low as 0.020 μM in a homogeneous time-resolved fluorescence enzymatic assay. VEGFR-2 active compounds display good activity against VEGFR-1 as well.