5018-41-7Relevant articles and documents
Development of a Scalable Synthesis of 4-Aminopyrimidin-5-ol, a Versatile Intermediate
Le, Phuong T.,Richardson, Paul F.,Sach, Neal W.,Xin, Shuibo,Ren, Shijian,Xiao, Jiezhan,Xue, Liangliang
, p. 639 - 645 (2015)
A robust process for the preparation of multigram quantities of 4-aminopyrimidin-5-ol (5) in good yield from an inexpensive and readily available pyrimidine starting material is described. An initial evaluation of the reported literature route for this material utilizing a de novo pyrimidine synthesis provided safety concerns over the scalability of several intermediates. In addition, a number of steps proceeded in mediocre yield, and involved chromatographic separations for the desired products. The newly developed route mitigates the safety concerns, reduces the number of steps from five to three, avoids column chromatography, leads to an 8-fold improvement in yield, and utilizes reagents, which are recognized to be more environmentally benign.
Pyrazole spleen tyrosine kinase inhibitor as well as preparation method and application thereof
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Paragraph 0449-0452, (2020/12/29)
The invention discloses a pyrazole spleen tyrosine kinase inhibitor, a preparation method thereof, a pharmaceutical composition containing the same, and application of the pyrazole spleen tyrosine kinase inhibitor and the pharmaceutical composition in the preparation of drugs for treating Syk-mediated diseases including cancers, inflammatory diseases and the like.
Pyrimidomorpholine derivative, and preparation method and application thereof
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Paragraph 0209; 0210; 0211, (2018/07/07)
The invention specifically relates to a small molecule compound capable of resisting medullary thyroid carcinoma, acute leukemia and inflammations, and a preparation method and application thereof, belonging to the field of chemical pharmaceuticals. The objective of the invention is to overcome the technical problems of poor selectivity, easy incurrence of drug resistance and toxic and side effectof conventional commercially-available clinical medicines for medullary thyroid carcinoma. The invention provides a pyrimidomorpholine derivative to overcome the above technical problem. The pyrimidomorpholine derivative is mainly characterized in that the position 6 of pyrimidine is substituted, and the structure of the pyrimidomorpholine is as shown in a formula I which is described in the specification. The compound provided by the invention has the advantages of high activity in resisting medullary thyroid carcinoma, low toxic and side effect and capacity of overcoming clinical drug resistance, and has great value in development of medicines for treating medullary thyroid carcinoma.