Triethylamine → HCID 131711697, 화합물

HRID 2052272노트

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HRID 2052272 반응식
[NH2:1][C@H:2]([C:7]([NH:9][C@H:10]([C:15]([NH:17][C@@H:18]([C:25]([NH2:27])=[O:26])[C:19]1[CH:24]=[CH:23][CH:22]=[CH:21][CH:20]=1)=[O:16])[CH2:11][C:12](=[O:14])[OH:13])=[O:8])[CH2:3][CH2:4][CH2:5][CH3:6].Cl.[NH:29]([C:51]([O:53][C:54]([CH3:57])([CH3:56])[CH3:55])=[O:52])[C@H:30]([C:41](ON1C(=O)CCC1=O)=[O:42])[CH2:31][C:32]1[C:40]2[C:35](=[CH:36][CH:37]=[CH:38][CH:39]=2)[NH:34][CH:33]=1.C(N(CC)CC)C>CN(C=O)C>[NH:29]([C:51]([O:53][C:54]([CH3:57])([CH3:56])[CH3:55])=[O:52])[C@H:30]([C:41]([NH:1][C@H:2]([C:7]([NH:9][C@H:10]([C:15]([NH:17][C@@H:18]([C:25]([NH2:27])=[O:26])[C:19]1[CH:20]=[CH:21][CH:22]=[CH:23][CH:24]=1)=[O:16])[CH2:11][C:12](=[O:13])[OH:14])=[O:8])[CH2:3][CH2:4][CH2:5][CH3:6])=[O:42])[CH2:31][C:32]1[C:40]2[C:35](=[CH:36][CH:37]=[CH:38][CH:39]=2)[NH:34][CH:33]=1

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 98767Boc-Trp-OSuHCID 131711698HCID 131711698, 화합물

생성물 1

HCID 131711697HCID 131711697, 화합물수율 97.5%

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

1.57 g (3.78 mmoles of H-Nle-Asp-D-Phg-NH2.HCl are reacted with 1.52 g (3.78 mmoles) of BOC-Trp-OSu in 50 ml of DMF in the presence of 1.06 ml (7.6 mmoles) of triethylamine. Next day the reaction mixture is evaporated in vacuo, the residue is admixed with water, and the suspension is filtered. 2.45 g (97.5%) of BOC-Trp-Nle-Asp-D-Phg-NH2 are obtained; m.p.: 217° C. (decomposition), Rf5 :0.35, [α]D -32.7° (c: 1.0, in dimethyl formamide).

후처리

  1. customNext day the reaction mixture is evaporated in vacuo
  2. filtrationthe suspension is filtered

출처 및 근거

ORD 기록
ord-ac74d92dc2fd4bc9bc97c3c08675c019
출처 데이터셋
uspto-grants-1980_01
특허 번호
US04183909

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