Novel tricyclic diamines 1. Synthesis of 1,4-diazaisotwistane and 1,4-diazahomoisotwistane as constrained 3-aminoquinuclidine isosteres |
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| Authors: | Ivar M. McDonald Alicia Ng Jingfang Cutrone Robert Mate Richard E. Olson |
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| Affiliation: | 1. Bristol-Myers Squibb, Drug Discovery, Wallingford, CT 06492, USA;2. Bristol-Myers Squibb, Drug Product Science & Technology, Princeton, NJ 08543, USA |
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| Abstract: | Synthesis of the novel tricyclic diamines 1,4-diazaisotwistane and 1,4-diazahomoisotwistane are described. These compact tricyclic cores have one tertiary and one secondary amine and may serve as ring-constrained isosteres of 3-aminoquinuclidine. Both tricycles were prepared by a similar strategy involving saturation of an appropriately substituted aromatic azaindole, functionalization and intramolecular alkylation. |
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| Keywords: | Diazaisotwistane Diazahomoisotwistane Tricyclic diamine Intramolecular cyclization 3-Aminoquinuclidine |
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