Dicyclohexylcarbodiimide → Urea

HRID 963121

反応式

HRID 963121 の反応式
N[C@H](C(N[C@H](C(N[C@H]([C:20]([NH:22][C@H](C(O)=O)C)=[O:21])CC(C)C)=O)C)=O)CC(C)C.[CH:28]1[C:33]([C:34]([NH:36][C@H:37]([C:43]([OH:45])=[O:44])[CH2:38][CH2:39][C:40]([OH:42])=[O:41])=[O:35])=[CH:32][CH:31]=[C:30]([NH:46][CH2:47][C:48]2[CH:49]=[N:50][C:51]3[N:57]=[C:56]([NH2:58])[N:55]=[C:54]([NH2:59])[C:52]=3[N:53]=2)[CH:29]=1.C1([N:66]=C=NC2CCCCC2)CCCCC1>CN(C)C=O>[CH:32]1[C:33]([C:34]([NH:36][C@H:37]([C:43]([OH:45])=[O:44])[CH2:38][CH2:39][C:40]([OH:42])=[O:41])=[O:35])=[CH:28][CH:29]=[C:30]([NH:46][CH2:47][C:48]2[CH:49]=[N:50][C:51]3[N:57]=[C:56]([NH2:58])[N:55]=[C:54]([NH2:59])[C:52]=3[N:53]=2)[CH:31]=1.[NH2:66][C:20]([NH2:22])=[O:21]

参加物

6

反応物 3

HCID 10868DicyclohexylcarbodiimideHCID 169371AminopterinHCID 53729605Leu-Ala-Leu-Ala3 回

生成物 2

HCID 1176UreaHCID 169371Aminopterin

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒2 回

実験手順

Conjugation Via Leu-Ala-Leu-Ala Spacer: The N-hydroxysuccinimide ester of aminopterin was prepared as above. To 10.2 ml of a 23 mM solution of the aminopterin derivative (0.236 mmol) in dimethylformamide were added 104 mg (0.236 mmol) of solid L-Leu-L-Ala-L-Leu-L-Ala (LALA). The mixture was stirred overnight at 50° C. during which time the solid LALA dissolved. To the reaction mixture was added 48.7 mg (0.236 mmol) of dicyclohexylcarbodiimide in 0.58 ml of dimethylformamide. Copious quantities of urea formed within 2 hours at room temperature and were removed by filtration. The filtrate containing the N-hydroxy succinimide ester of the LALA derivative of aminopterin was retained.

後処理

  1. dissolutiondissolved

出典と根拠

ORDレコード
ord-afe15a1e8c3b43d98e880078b9d752de
出典データセット
uspto-grants-1998_06
特許番号
US05762918

関連ノート

読み込み中…