Pamoic Acid → Octreotide pamoate

HRID 1735639

反応式

HRID 1735639 の反応式
[CH3:1][C@@H:2]([OH:71])[C@@H:3]1[NH:27][C:25](=[O:26])[C@H:24]([CH2:28][CH2:29][CH2:30][CH2:31][NH2:32])[NH:23][C:21](=[O:22])[C@@H:20]([CH2:33][C:34]2[C:38]3[CH:39]=[CH:40][CH:41]=[CH:42][C:37]=3[NH:36][CH:35]=2)[NH:19][C:17](=[O:18])[C@H:16]([CH2:43][C:44]2[CH:45]=[CH:46][CH:47]=[CH:48][CH:49]=2)[NH:15][C:13](=[O:14])[C@@H:12]([NH:50][C:51]([C@H:53]([NH2:61])[CH2:54][C:55]2[CH:56]=[CH:57][CH:58]=[CH:59][CH:60]=2)=[O:52])[CH2:11][S:10][S:9][CH2:8][C@@H:7]([C:62]([NH:64][C@@H:65]([C@H:68]([OH:70])[CH3:69])[CH2:66][OH:67])=[O:63])[NH:6][C:4]1=[O:5].[CH:72]1[CH:77]=[C:76]2[CH:78]=[C:79]([C:98]([OH:100])=[O:99])[C:80]([OH:97])=[C:81]([CH2:82][C:83]3[C:92]4[C:87](=[CH:88][CH:89]=[CH:90][CH:91]=4)[CH:86]=[C:85]([C:93]([OH:95])=[O:94])[C:84]=3[OH:96])[C:75]2=[CH:74][CH:73]=1>O.O1CCOCC1>[CH3:1][C@@H:2]([OH:71])[C@@H:3]1[NH:27][C:25](=[O:26])[C@H:24]([CH2:28][CH2:29][CH2:30][CH2:31][NH2:32])[NH:23][C:21](=[O:22])[C@@H:20]([CH2:33][C:34]2[C:38]3[CH:39]=[CH:40][CH:41]=[CH:42][C:37]=3[NH:36][CH:35]=2)[NH:19][C:17](=[O:18])[C@H:16]([CH2:43][C:44]2[CH:49]=[CH:48][CH:47]=[CH:46][CH:45]=2)[NH:15][C:13](=[O:14])[C@@H:12]([NH:50][C:51]([C@H:53]([NH2:61])[CH2:54][C:55]2[CH:60]=[CH:59][CH:58]=[CH:57][CH:56]=2)=[O:52])[CH2:11][S:10][S:9][CH2:8][C@@H:7]([C:62]([NH:64][C@@H:65]([C@H:68]([OH:70])[CH3:69])[CH2:66][OH:67])=[O:63])[NH:6][C:4]1=[O:5].[CH:72]1[CH:73]=[CH:74][C:75]2[C:76](=[CH:78][C:79]([C:98]([OH:100])=[O:99])=[C:80]([OH:97])[C:81]=2[CH2:82][C:83]2[C:84]([OH:96])=[C:85]([C:93]([OH:95])=[O:94])[CH:86]=[C:87]3[C:92]=2[CH:91]=[CH:90][CH:89]=[CH:88]3)[CH:77]=1

参加物

4

反応物 2

HCID 8546Pamoic AcidHCID 448601Octreotide2 回

生成物 1

HCID 44194024Octreotide pamoate

試薬・触媒・溶媒 1

HCID 218864351,4-Dioxane--water (1/1)溶媒

実験手順

10.19 g of octreotide free base (10 mM) and 3.88 embonic acid (10 mM) are dissolved in 1 liter of water/dioxane (1:1). The reaction mixture is filtered, and lyophilized to give a yellow powder [α]20D=+7.5° (C=0.35, in DMF), of octreotide pamoate hydrate. Factor=1.4 wherein the factor=weight of lyophilizate/weight of octreotide contained therein.

後処理

  1. filtrationThe reaction mixture is filtered
  2. customto give a yellow powder [α]20D=+7.5° (C=0.35, in DMF)

出典と根拠

ORDレコード
ord-b47e8b278e13464894097467ad20f6c6
出典データセット
uspto-grants-1996_07
特許番号
US05538739

関連ノート

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