Stereoselective intramolecular cycloadditions of homochiral nitrile imines: synthesis of enantiomerically pure 3,3a-dihydro-pyrazolo[1,5-a][1,4]benzodiazepine-6(4H)-ones期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Stereoselective intramolecular cycloadditions of homochiral nitrile imines: synthesis of enantiomerically pure 3,3a-dihydro-pyrazolo[1,5-a][1,4]benzodiazepine-6(4H)-ones

Affiliation:	1. Dipartimento di Chimica Organica e Industriale, Università di Milano, via Golgi 19, 20133 Milano, Italy;2. Dipartimento di Scienze Chimiche, Fisiche e Matematiche, Università dell''Insubria, via Lucini 3, 22100 Como, Italy;3. Consiglio Nazionale delle Ricerche, Centro per lo Studio delle Relazioni tra Struttura e Reattività Chimica, via Golgi 19, 20133 Milano, Italy;1. Shanghai Key Laboratory of New Drug Design & School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China;2. College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, PR China;1. Normandie Univ, INSA Rouen, UNIROUEN, CNRS, COBRA (UMR 6014), 76000 Rouen, France;2. Institut Universitaire de France, 1 rue Descartes, 75231 Paris, France

Abstract:	Starting from the commercially available (S)-1-phenylethylamine, we have synthesised the homochiral hydrazonoyl chlorides 4. The intramolecular cycloaddition of the corresponding nitrile imines 5 gave the diastereoisomeric 3,3a-dihydro-pyrazolo[1,5-a][1,4]benzodiazepine-6(4H)-ones 6 and 7 in enantiopure form.

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