反応式
[NH:1]([C:17]([O:19]C(C)(C)C)=O)[C@H:2]([C:14]([OH:16])=O)[CH2:3][C:4](=[O:13])[O:5]CC1C=CC=CC=1.[NH:24](C(OC(C)(C)C)=O)[C@H:25](C(O)=O)[C@H:26]([CH2:28][CH3:29])[CH3:27].[NH:40]([C:55]([O:57][C:58]([CH3:61])([CH3:60])[CH3:59])=[O:56])[C@H:41]([C:52]([OH:54])=O)[CH2:42][CH2:43][CH2:44][NH:45][C:46](=[NH:51])[NH:47][N+]([O-])=O.[NH2:62][C@H:63]([C:74]([NH:76][C@H:77]([C:82]([NH:84][CH2:85][C:86]([O:88]C)=O)=[O:83])[C@H:78]([CH2:80][CH3:81])[CH3:79])=[O:75])[CH2:64][CH2:65][CH2:66][NH:67][C:68](=[NH:73])[NH:69][N+]([O-])=O.FC(C(O)=O)(F)F.[NH2:97][NH2:98]>>[NH:40]([C:55]([O:57][C:58]([CH3:61])([CH3:60])[CH3:59])=[O:56])[C@H:41]([C:52]([NH:24][C@H:25]([C:17]([NH:1][C@H:2]([C:14]([NH:62][C@H:63]([C:74]([NH:76][C@H:77]([C:82]([NH:84][CH2:85][C:86]([NH:97][NH2:98])=[O:88])=[O:83])[C@H:78]([CH2:80][CH3:81])[CH3:79])=[O:75])[CH2:64][CH2:65][CH2:66][NH:67][C:68](=[NH:73])[NH2:69])=[O:16])[CH2:3][C:4](=[O:13])[OH:5])=[O:19])[C@H:26]([CH2:28][CH3:29])[CH3:27])=[O:54])[CH2:42][CH2:43][CH2:44][NH:45][C:46](=[NH:51])[NH2:47]参加物
実験手順
The hexapeptide fragment containing the amino acid residues Nos. 16-21 is prepared as follows. The tripeptide fragment containing residues Nos. 19-21 is prepared by the solid-phase method as described above, cleaved from the resin support with MeOH-TEA and treated with trifluoroacetic acid (TFA) to obtain the corresponding methyl ester as the TFA salt, H-Arg(NO2)-Ile-Gly-OCH3.TFA (9). The amino acids corresponding to residues No. 18 (as Boc-Asp(Bzl)-OH), No. 17 (as Boc-Ile-OH.1/2H2O), and No. 16 (as Boc-Arg(NO2)-OH) are then coupled in succession to the above tripeptide (9) by classical methods. The resulting protected hexapeptide methyl ester is deprotected and treated with hydrazine to obtain the corresponding Boc-hexapeptide hydrazide as the acetate salt, Boc-Arg-Ile-Asp-Arg-Ile-Gly-NHNH2.2HOAc (16).
出典と根拠
- ORDレコード
- ord-e6143db145864fc4a161d3c1b48a6342
- 出典データセット
- uspto-grants-1986_08
- 特許番号
- US04607023
関連ノート
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