Synthesis of a highly potent analog of luteinizing hormone releasing hormone (LH-RH): (Des-Gly-NH210, pro-NH-Et9)-LH-RH.

• 品川 進

• 藤野 政彦

抄録

A highly potent analog of luteinizing hormone releasing hormone (LH-RH), pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-NHCH₂-CH₃ was synthesized by the conventional solution method. The key intermediate, H-Leu-Arg (NO₂)-Pro-NHCH₂-CH₃, which was prepared by the stepwise manner using the activated esters of the corresponding protected amino acids, was coupled with N-terminal hexapeptide, pGlu-His-Trp-Ser-Tyr-Gly-OH, by the HONB/DCC method to give the mono-protected nonapeptide ethylamide. The protected peptide was treated with stannous chloride in 60% aqueous formic acid to remove the nitro group. The purification of the resulting peptide was carried out by a column chromatography on Amberlite XAD-2 and followed by a column chromatography on carboxymethylcellulose. The synthetic method described is promising for preparing this analog of LH-RH in large quantities and good quality.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 23 (1), 229-232, 1975

  公益社団法人 日本薬学会

キーワード

• Drug Discovery
• General Chemistry
• General Medicine

詳細情報

• CRID: 1390001204173485952
• NII論文ID: 110003621670
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.23.229
• ISSN: 13475223
• ISSN: 00092363
• PubMed: 1100284
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/23/1/23_1_229/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1975084704
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可