An Efficient Synthesis of 6-Substituted Aminohexahydro-1H-1,4-diazepines from 2-Substituted Aminopropenals.
書誌事項
- タイトル別名
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- Efficient Synthesis of 6 Substituted Am
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抄録
Swern oxidation of 2-substituted amino-1, 3-propanediols 20a-d, 38, 41, and 42 smoothly proceeded to give the oxidative dehydration products, 2-substituted aminopropenals 17a-d, 43, 45 and 46, respectively. Reaction of the intriguing 2- substituted aminopropenals 17a-d with N-benzyl-N'-methyl- or N, N'-dimethylethylenediamine(12o or 12p) followed by NaBH4 reduction of the iminium salt intermediates afforded the corresponding 6-substituted aminohexahydro-1H-1, 4-diazepines 16 and 24-28. The similar ring formation of 1H-indazole derivatives 43 and 45 employing 12o directly furnished the 1H-dindazole-3-carboxamide 4, which showed a potent serotonin-3(5-HT3) receptor antagonistic activity.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 44 (12), 2205-2212, 1996
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679141179776
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- NII論文ID
- 130003773370
- 110003631844
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DyaK2sXitFymtQ%3D%3D
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- ISSN
- 13475223
- 00092363
- http://id.crossref.org/issn/00092363
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- NDL書誌ID
- 4098946
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可