Selective ring N-protection of aminopyrazoles

被引:11
作者
Seelen, W
Schäfer, M
Ernst, A
机构
[1] Schering AG, Res Ctr Europe, Med Chem, D-13342 Berlin, Germany
[2] Schering AG, Res Ctr Europe, Struct Biol, D-13342 Berlin, Germany
关键词
D O I
10.1016/S0040-4039(03)00988-2
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Two simple Procedures for the selective protection of the ring N of aminopyrazoles as tert-butoxycarbamate (Boc) in high yields are reported: several other protecting groups (Cbz, Bn. SEM) can be introduced using the one-pot procedure (method B). The N-Boc protected aminopyrazoles are acylated at the exocyclic NH2 group and subsequently deprotected to give the corresponding 3-acylaminopyrazoles in high yields. This procedure is applicable for the rapid parallel synthesis of 3-acylaminopyrazoles. (C) 2003, Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:4491 / 4493
页数:3
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