Thiazole analogs of benzomorphans. I. Synthesis of novel thiazolo(4,5-f)morphans.

• 勝浦 公男

• 太田 雅夫

• 三橋 監物

抄録

The synthesis and analgesic properties of thiazolo [4, 5-f] morphans (XIIa-c) are described. Monothiazolization of ethyl 2-methyl-1, 3-dioxo-2-cyclohexaneacetate (I) afforded the 2-aminothiazole derivative (II), which was deaminated to ethyl 4, 5, 6, 7-tetrahydro-4-methyl-5-oxo-4-benzothiazoleacetate (V) by means of the Sandmeyer reaction and subsequent hydrogenolysis of the resulting chloride (IVa). In several steps, V was converted to 2, 5-dimethyl-9-oxothiazolo [4, 5-f] morphan (X). Thiazolo [4, 5-f] morphan derivatives (XIIa-c) were synthesized from this key intermediate (X).

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 30 (12), 4378-4383, 1982

  公益社団法人 日本薬学会

キーワード

• thiazolo [4, 5-f] morphan

詳細情報

• CRID: 1390001204164670080
• NII論文ID: 130003769040
• DOI: 10.1248/cpb.30.4378
• ISSN: 13475223
• ISSN: 00092363
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/30/12/30_12_4378/_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