发明名称 DEPROTECTION OF AMINO GROUP AND HYDROXY GROUP PROTECTED WITH ALKYNYLMETHYLOXYCARBONYL GROUP
摘要 PROBLEM TO BE SOLVED: To efficiently deprotect an amino group and a hydroxy group protected with an alkynylmethyloxycarbonyl group by bonding the amino group and the hydroxy group with the alkynylmethyloxycarbonyl group, by allowing a strong acid to act on the protected groups in the presence of a metal or a metal complex to isolate the amino group or the hydroxy group. SOLUTION: For example, in the reaction formula (R is H, an alkyl or the like, R1 is a sugar derivative or the like; R2 and R3 are each H, an amino acid derivative or the like), when an alkynylmethyl chlorocarbonate of structure 1 is reacted with an alcohol 2a or an amine 2b, a corresponding alkynylmethyloxycarbonyl derivative 3a or 3b is formed, and the hydroxy group and the amino group is protected. When a strong acid such as trifluoroacetic acid(TFA) is allowed to act on the obtained alkynylmethyloxycarbonyl derivative 3a or 3b in the presence of a cobalt carbonyl complex, the deprotection is rapidly and efficiently carried out to regenerate the original alcohol 2a or amine 2b.
申请公布号 JP2000186049(A) 申请公布日期 2000.07.04
申请号 JP19980364340 申请日期 1998.12.22
申请人 UNIV OSAKA 发明人 KUSUMOTO SHOICHI;FUKASE KOICHI
分类号 C07B51/00;C07B61/00;(IPC1-7):C07B51/00 主分类号 C07B51/00
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