| 摘要 |
<p>PURPOSE: Provided is a method for producing vinylpyrimidine in excellently high yield by vinylation of a pyrimidine derivative using a vinylborane compound so as to improve both economical and environmental problems. CONSTITUTION: The vinylpyrimidine of formula(I) is produced by the steps of: reacting a compound of the formula(II) with borane compound in the presence of Pd complex; additionally reacting a product of the formula(I) (wherein, R2 is hydrogen) with a compound of the formula(IV) in the presence of Lewis acid. In the formula(I), R1 is hydrogen or carboxylester group, and R is hydrogen or a group of formula(a)(wherein, Ra is hydrogen, a protective group or a hydrolyzable group under physiological condition. In the formula(II), R21 is hydrogen or a group of formula(a)(wherein, a hydroxy group can be protected), R3 is bromo, chloro or iodo, and R1 is described as in the above. In the formula(IV), Rb is a protective grop of hydroxy group and Z is a leaving group.</p> |
