84955-32-8Relevant academic research and scientific papers
Compound with 2-aminopyrimidine structure as well as preparation method and purpose thereof
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Paragraph 0174-0177, (2019/06/08)
The invention provides a compound of a 2-aminopyrimidine structure shown as a general formula (1), or a stereisomer, enantiomers or medically acceptable salt of the compound, a preparation method of the compound, a medicine composition containing the composition or a purpose of the composition. The compound shown as the general formula (1) can be used for preparing NIK kinase inhibitors, and can be used for preventing and/or treating diseases relevant to NIK kinase, particularly cancer and metabolic diseases, such as B-cell dysfunction related cancer such as multiple myeloma, lymphocyte carcinoma, diffuse large B cell lymphoma of liver cancer, hodgkin lymphoma and chronic lymphocytic leukemia, prostatic cancer, liver cancer, intestinal cancer, medicine induced liver damage, alcohol inducedliver damage, toxic induced acute liver injury, chronic liver inflammation and the like. The general formula (1) is shown in the description.
THE SYNTHESIS OF N-PYRIMIDIN-5-YL)ETHYL>BENZOYL>-L-GLUTAMIC ACIDS AS ANTINEOPLASTIC AGENTS
Shih, Chuan,Gossett, L. S.
, p. 825 - 841 (2007/10/02)
A series of N-pyrimidin-5-yl)ethyl>benzoyl>-L-glutamic acids were synthesized.In this current synthesis, compound 2-amino-4-chloro-pyrrolopyrimidine (4) was selected as an important precursor for the preparation of key intermediates such as 5b, 10b, 15a and 15b.These highly functionalized pyrrolopyrimidines were then later coupled with either 4-ethynylbenzoylglutamate or 4-iodobenzoylglutamate in a palladium catalyzed Heck reaction and thus provided the basic skeleton of the targeted molecules.The availability ofthe chlorine atom at the 4-position of the pyrrolopyrimidine nucleus has allowed us to introduce different substituents at this position efficiently.By this approach, we were able to prepare a variety of 4-substituted pyrrolopyrimidine based folate antagonists (2a-2g) which are closely related to the novel thymidylate synthase inhibitor LY231514.In vitro analysis has demonstrated that some of these agents are highly cytotoxic against human leukemic cells (CCRF-CEM) in culture.
Synthesis of Acyclo-7-deazaguanosine by Regiospecific Phase-Transfer Alkylation of 2-Amino-4-methoxy-7H-pyrrolopyrimidine
Seela, Frank,Kehne, Andreas,Winkeler, Heinz-Dieter
, p. 137 - 146 (2007/10/02)
Acyclo-7-deazaguanosine (2), a structural analogue of the antiviral highly active acycloguanosine (1), has been synthesized.Regiospecificity of the electrophilic attack was shown by phase-transfer methylation of 2-amino-4-methoxy-7H-pyrrolopyrimidi
