发明名称 METHOD FOR ELIMINATING PROTECTING GROUP
摘要 PURPOSE:To eliminate a protecting group and obtain the objective substance in good yield by reacting a compound having amino, hydroxyl, SH group, etc., protected with benzyloxycarbonyl, benzyl group, etc., with zinc in a buffer solution. CONSTITUTION:A compound having NH2, OH or SH group protected with (substituted) benzyloxycarbonyl group or NH2, OH, SH or COOH group protected with (substituted) benzyl group is reacted with zinc in a buffer solution at ambient temperature to eliminate the protecting group. A phosphoric acid, acetic acid or N-methylmorpholine buffer solutions, etc., in 0.3-1.0mol concentration are used as the buffer solution to keep the pH of the reaction system at 6-7. In order to ensure a homogeneous reaction system, an organic solvent (e.g., THF) without affecting the reaction, as necessary, can be also used. Not only zinc in the form of a simple substance but also zinc-copper powder, zinc amalgam, etc., may be used as the zinc in an amount of 1.5-2.5 times based on the substance to be reacted.
申请公布号 JPH02714(A) 申请公布日期 1990.01.05
申请号 JP19880090233 申请日期 1988.04.14
申请人 LEDERLE JAPAN LTD 发明人 AOYANAGI SAKAE;HAYASHI TAKAAKI;KURAMOTO YASUHIRO
分类号 C07D285/06;C07B41/02;C07B41/08;C07B43/04;C07B45/06;C07B51/00;C07D231/04;C07D477/00;C07D487/04;C07D501/36 主分类号 C07D285/06
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