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    • 5. 发明授权
    • Liquid phase process for the preparation of GnRH peptides
    • 用于制备GnRH肽的液相方法
    • US5977302A
    • 1999-11-02
    • US195049
    • 1998-11-18
    • David C. PalmerAhmed Abdel-MagidMichael S. BreslavUrs P. EggmannBruce HarrisMark L. HaslegoKirk L. Sorgi
    • David C. PalmerAhmed Abdel-MagidMichael S. BreslavUrs P. EggmannBruce HarrisMark L. HaslegoKirk L. Sorgi
    • C07K5/09C07K5/103C07K5/107C07K7/23C07K7/06
    • C07K5/0815C07K5/101C07K5/1013C07K5/1016C07K7/23Y02P20/55
    • A liquid phase process for preparing GnRH peptide analogs of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)-AA.sub.5 -AA.sub.6 AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2Formula 1which comprises:(a) reacting a peptide of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -Xwhere T is (P.sub.2)AA4 orP.sub.2 and X is AA.sub.7 --OH or is --OH, with a peptide of the formula:X'-AA.sub.8 -Pro-AA.sub.10 -NH.sub.2or acid-addition salt form thereof, where X' is AA.sub.7 when X is absent and X' selected from P-Ala, Gly, GABA, the D- and L- isomers of Ala, amino isobutyric acid, 6-amino-hexanoic acid, Ser, Thr, His, Tyr, Asn, and Gln' is absent when X is AA.sub.7 --OH;in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2(b) removing the P.sub.2 protecting group at the N-terminus, and(c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula:G-AA.sub.1 -(R.sub.1)D-Phe-AA.sub.3 -T'or acid-addition salt form thereof, where T' is AA.sub.4 --OH when T is absent and is absent when T is P2-AA.sub.4, in a liquid reaction medium to obtain a GnRH peptide of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2.
    • 用于制备下式的GnRH肽类似物的液相方法:G-AA1-(A)D-Phe-AA3-AA4-(R2)-AA5-AA6AA7-AA8-Pro-AA10-NH2式1,其包含:(a )使下式的肽与下式的肽反应:其中T是(P2)AA4或P2,X是AA7-OH或-OH的式(T-(R2)AA5-AA6-X)肽与下式的肽反应:X'-AA8-Pro -AA10-NH2或其酸加成盐形式,其中当X不存在时X'为AA 7,X'选自P-Ala,Gly,GABA,Ala的D-和L-异构体,氨基异丁酸, 当X是AA7-OH时,氨基己酸,Ser,Thr,His,Tyr,Asn和Gln'不存在; 在液体反应介质中,在肽偶联剂和强有机胺碱的存在下,得到下式的产物:((R 2)AA 5 -A AA 6 -A AA 7 -A AA 8 -Pro-AA 10 -NH 2(b) P2保护基团,和(c)使步骤(b)的产物或其酸加成盐与下式的肽反应:G-AA1-(R1)D-Phe-AA3-T' 或其酸加成盐形式,其中当T不存在时T'为AA4-OH,当T为P2-AA4时不存在,在液体反应介质中得到G-AA1 - (A)的GnRH肽, D-Phe-AA3-AA4-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2。
    • 6. 发明授权
    • Liquid phase process for the preparation of GNRH peptides
    • 用于制备GNRH肽的液相方法
    • US06235876B1
    • 2001-05-22
    • US09350231
    • 1999-07-08
    • David C. PalmerAhmed Abdel-MagidUrs P. EggmannBruce HarrisKirk L. Sorgi
    • David C. PalmerAhmed Abdel-MagidUrs P. EggmannBruce HarrisKirk L. Sorgi
    • C07K704
    • C07K5/0815C07K5/101C07K5/1013C07K5/1016C07K7/23Y02P20/55
    • A liquid phase process for preparing GnRH peptide analogs of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2-AA5-AA6-AA7-AA8-Pro-AA10-NH2   Formula 1 which comprises: (a) reacting a peptide of the formula: T-(R2)AA5-AA6-X  where T is (P2) AA4 orP2 and X is AA7-OH or is —OH, with a peptide of the formula: X′-AA8-Pro-AA10-NH2  or acid-addition salt form thereof, where X′ is AA7 when X is absent and X′ is absent when X is AA7-OH;  in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula: T-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2 (b) removing the P2 protecting group at the N-terminus, and (c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula: G-AA1-(R1)D-Phe-AA3-T′  or acid-addition salt form thereof, where T′ is AA4-OH when T is absent and is absent when T is P2-AA4, in a liquid reaction medium to obtain a GnRH peptide of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2.
    • 用于制备下式的GnRH肽类似物的液相方法:其包括:(a)使下式的肽与其中T是(P2)AA4或P2,X是AA7-OH或-OH的肽反应, 式:或其酸加成盐形式,其中当X不存在时X'为AA 7,X为AA 7 -OH时X'不存在; 在液体反应介质中,在肽偶联剂和强有机胺碱存在下,得到下式的产物:(b)在N末端除去P2保护基,和(c)使步骤 (b)或其酸加成盐与下式的肽或其酸加成盐形式,当T不存在时T'为AA4-OH,当T为P2-AA4时不存在,在液体反应中 培养基以获得下式的GnRH肽: