Aqueous phosphoric acid as a mild reagent for deprotection of the t-butoxycarbonyl group

被引:38
作者
Li, B [1 ]
Bemish, R
Buzon, RA
Chiu, CKF
Colgan, ST
Kissel, W
Le, T
Leeman, KR
Newell, L
Roth, J
机构
[1] Pfizer Global Res & Dev, Chem Res & Dev, Groton Labs, Groton, CT 06340 USA
[2] Pfizer Global Res & Dev, Chem Res & Dev, Holland, MI 49424 USA
关键词
phosphoric acid; BOC; deprotection;
D O I
10.1016/j.tetlet.2003.09.040
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Aqueous phosphoric acid (85 wt%) is an efficient and mild reagent for the deprotection of N-BOC groups. Acid sensitive functionalities including benzyl and methyl esters, TBDMS ether, CBZ and isopropylidene groups are compatible with the reaction conditions. The reactions are high yielding, and the workup is convenient. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:8113 / 8115
页数:3
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