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METHODS OF PREPARATION AND RESOLUTION OF E/Z ISOMERS OF VINYLFURO2,3-D PYRIMIDINE AND THEIR BIOLOGICAL ACTIVITIES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT
METHODS OF PREPARATION AND RESOLUTION OF E/Z ISOMERS OF VINYLFURO2,3-D PYRIMIDINE AND THEIR BIOLOGICAL ACTIVITIES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT
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机译:乙烯基[2,3-D]嘧啶的E / Z异构体的制备和拆分方法及其生物学活性,组成和治疗方法
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摘要
Stereoselective methods for preparing the individual isomers, E- and Z-2,4-substituted-5-vinylfuro[2,3-d]pyrimidine and pharmaceutically acceptable salts, solvates, and prodrugs thereof using selective synthetic conditions are provided. This class of pyrimidine compounds function as receptor tyrosine kinase inhibitors during angiogenesis and resists the development of new blood vessels in tumors as well as inhibit the folate pathway required for cell growth. The isomers of these compounds are separated by physical, chromatographic, and/or HPLC methods. Their biological activities are described. Also provided are methods of treating diseases associated with angiogenesis in a patient comprising administering the isolated E- and Z- isomers of the composition of the present invention.
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