Rapid synthesis of tetrahydro-4H-pyrazolo[1,5-a]diazepine-2-carboxylate

被引:22
|
作者
Cvetovich, RJ [1 ]
Pipik, B [1 ]
Hartner, FW [1 ]
Grabowski, EJJ [1 ]
机构
[1] Merck & Co Inc, Merck Sharp & Dohme Res Labs, Dept Proc Res, Rahway, NJ 07065 USA
关键词
aminohydrazines; hydroxyhydrazines; pyrazole formation; pyrazolo-diazepine;
D O I
10.1016/S0040-4039(03)01417-5
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Hydrazines condense with dimethyl 2-pyrrolidino-4-oxo-2-pentenedioate in the presence of aq. HCl to form N-substituted pyrazole-3,5-dicarboxylates 2. Complex bicyclic derivatives, such as pyrazolo-oxazine 3a, pyrazolo-oxazepine 3b, pyrazolopyrazine 4a, and pyrazolo-diazepine 4b, were generated using 2-hydrazinoethanol, 3-hydrazinopropanol, 2-hydrazinoethylamine, and 3-hydrazinopropylamine. (C) 2003 Elsevier Ltd. All rights reserved.
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页码:5867 / 5870
页数:4
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