Synthesis of 1,2-Disubstituted-1-carbacephem
スポンサーリンク
概要
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Various kinds of 1,2-disubstituted-1-carbacephems were synthesized by employing several electrophilic reactions (e.g. oxidation, halogenation, halogenohydrination) toward the aldehyde 2 followed by cyclization, and also from 1,2-dehydro-1-carbacephem 10. The stereochemistry of the 1,2-disubstituted-1-carbacephems prepared was determined by proton nuclear magnetic resonance (^1H-NMR) analysis. The diol 4a, chlorohydrin 15a and bromohydrin 17a were converted to the corresponding 7-N-acylated compounds 27a-c. Antibacterial activities of 27a-c, however, were rather low compared with those of KT 3919 (non-substituted carbocephem) and KT 3933 (2α-hydroxy carbacephem), which are the racemates of KT 3767 and KT 3937,respctively.
- 社団法人日本薬学会の論文
- 1989-09-25
著者
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鈴木 文夫
Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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平田 正
Tokyo Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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斉藤 博満
Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories
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平田 正
Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories
-
鈴木 文夫
Kyowa Hakko Kogyo Co., Ltd., Tokyo Research Laboratories
-
斉藤 博満
Kyowa Hakko Kogyo Co. Ltd. Tokyo Research Laboratories
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