Studies on prodrugs. III. A convenient and practical preparation of ampicillin prodrugs.

• 池田 昇司

• 坂本 文夫

• 近藤 裕郷

• 森山 勝

• 塚本 悟郎

抄録

In order to prepare ampicillin prodrugs conveniently for practical use, a new synthetic method for 6β-aminopenicillanic acid (6-APA) esters as key intermediates of various ampicillin prodrugs has been developed. Acylation of 6-APA esters to ampicillin esters was achieved in good yields by using phenylglycyl chloride hydrochloride in dichloromethane in the presence of sodium bicarbonate and amide, or ammonium bicarbonate alone. KBT-1585, bacampicillin, talampicillin and pivampicillin have been obtained in good yields by this procedure.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 32 (11), 4316-4322, 1984

  公益社団法人 日本薬学会

キーワード

• acylation

詳細情報

• CRID: 1390001204163702528
• NII論文ID: 130003769474
• DOI: 10.1248/cpb.32.4316
• COI: 1:CAS:528:DyaL2MXhsVyqsbo%3D
• ISSN: 13475223
• ISSN: 00092363
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/32/11/32_11_4316/_pdf
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可