Triethylamine → 1-((2S)-2-(N-((1S)-1-Ethoxycarbonyl-3-phenylpropyl)amino)propionyl)-4-(2,3-dichloro-4-((ethoxycarbonyl)methoxy)benzoyl)methyleneproline ethyl ester

HRID 579734노트

반응식

HRID 579734 반응식
[CH2:1]([O:3][C:4]([C@@H:6]([N:15](C(OCC(Cl)(Cl)Cl)=O)[C@H:16]([C:18]([OH:20])=O)[CH3:17])[CH2:7][CH2:8][C:9]1[CH:14]=[CH:13][CH:12]=[CH:11][CH:10]=1)=[O:5])[CH3:2].[CH2:29]([O:31][C:32](=[O:56])[C@@H:33]1[CH2:37][C:36](=[CH:38][C:39](=[O:55])[C:40]2[CH:45]=[CH:44][C:43]([O:46][CH2:47][C:48]([O:50][CH2:51][CH3:52])=[O:49])=[C:42]([Cl:53])[C:41]=2[Cl:54])[CH2:35][NH:34]1)[CH3:30].C(N(CC)CC)C>C(Cl)Cl>[CH2:29]([O:31][C:32](=[O:56])[C@@H:33]1[CH2:37][C:36](=[CH:38][C:39](=[O:55])[C:40]2[CH:45]=[CH:44][C:43]([O:46][CH2:47][C:48]([O:50][CH2:51][CH3:52])=[O:49])=[C:42]([Cl:53])[C:41]=2[Cl:54])[CH2:35][N:34]1[C:18](=[O:20])[C@@H:16]([NH:15][C@H:6]([C:4]([O:3][CH2:1][CH3:2])=[O:5])[CH2:7][CH2:8][C:9]1[CH:10]=[CH:11][CH:12]=[CH:13][CH:14]=1)[CH3:17])[CH3:30]

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 13376527N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)-N-(2,2,2-trichloroethoxycarbonyl)alanineHCID 573200794-(2,3-Dichloro-4-((ethoxycarbonyl)methoxy)benzoyl)methylene proline ethyl ester

생성물 1

HCID 677408261-((2S)-2-(N-((1S)-1-Ethoxycarbonyl-3-phenylpropyl)amino)propionyl)-4-(2,3-dichloro-4-((ethoxycarbonyl)methoxy)benzoyl)methyleneproline ethyl ester

시약·촉매·용매 1

HCID 6344Dichloromethane용매2회

실험 절차

The acid chloride of N-((1S)-1-ethoxycarbonyl-3phenylpropyl)-N-(2,2,2-trichloroethoxycarbonyl)alanine (Example 7A) is dissolved in CH2Cl2 and added dropwise to a solution of 4-(2,3-dichloro-4-((ethoxycarbonyl)methoxy)benzoyl)methylene proline ethyl ester and triethylamine in CH2Cl2. Further reaction and purification as in example 7A gives the desired amide.

후처리

  1. customFurther reaction and purification as in example 7A

출처 및 근거

ORD 기록
ord-2ba06469a5484b4799245b00a0601fe7
출처 데이터셋
uspto-grants-1988_06
특허 번호
US04749698

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