A CONVENIENT METHOD FOR REGIOSELECTIVE C-5 HALOGENATION OF 4(3H)-OXO-7H-PYRROLO[2,3-D]PYRIMIDINES
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作者:
BARNETT, CJ
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机构:Chemical Process Research and Development Division, Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana
BARNETT, CJ
KOBIERSKI, ME
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机构:Chemical Process Research and Development Division, Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana
KOBIERSKI, ME
机构:
[1] Chemical Process Research and Development Division, Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana
N-7, O-Disilylation of 4(3H)-oxo-7H-pyrrolo[2,3-d]pyrimidines provides a convenient method for activation of these compounds toward regiospecific halogenation at C-5. The sequence is conveniently carried out without isolation of the silylated derivatives and desilylation is spontaneous upon addition of water to the reaction mixture.