(R)-tert-butyl 3-(3-fluorophenoxy)pyrrolidine-1-carboxylate → (R)-methyl 4-(1-(5-chloro-2-(3-(3-fluorophenoxy)pyrrolidin-1-yl)nicotinamido)cyclopropyl)benzoate

HRID 72543

반응식

HRID 72543 반응식
[F:1][C:2]1[CH:3]=[C:4]([CH:18]=[CH:19][CH:20]=1)[O:5][C@@H:6]1[CH2:10][CH2:9][N:8]([C:11](OC(C)(C)C)=O)[CH2:7]1.ClC1[N:43]=[CH:42][C:41]([Cl:44])=[CH:40][C:23]=1[C:24]([NH:26][C:27]1([C:30]2[CH:39]=[CH:38][C:33]([C:34]([O:36][CH3:37])=[O:35])=[CH:32][CH:31]=2)[CH2:29][CH2:28]1)=[O:25]>>[Cl:44][C:41]1[CH:42]=[N:43][C:11]([N:8]2[CH2:9][CH2:10][C@@H:6]([O:5][C:4]3[CH:18]=[CH:19][CH:20]=[C:2]([F:1])[CH:3]=3)[CH2:7]2)=[C:23]([CH:40]=1)[C:24]([NH:26][C:27]1([C:30]2[CH:31]=[CH:32][C:33]([C:34]([O:36][CH3:37])=[O:35])=[CH:38][CH:39]=2)[CH2:29][CH2:28]1)=[O:25]

참가 물질

3

반응물 2

HCID 67958316(R)-tert-butyl 3-(3-fluorophenoxy)pyrrolidine-1-carboxylateHCID 86697873Methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoate

생성물 1

HCID 67966692(R)-methyl 4-(1-(5-chloro-2-(3-(3-fluorophenoxy)pyrrolidin-1-yl)nicotinamido)cyclopropyl)benzoate수율 106.4%

실험 절차

The title compound (D205) (96 mg) was prepared according to the experimental procedure described in Description 160 starting from (R)-tert-butyl 3-(3-fluorophenoxy)pyrrolidine-1-carboxylate (D47) (100 mg, 0.355 mmol) and reacting in the second step with methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoate (D97) (D021/056/3) (65 mg, 0.177 mmol).

출처 및 근거

ORD 기록
ord-459729c531784e3c839137aab443158b
출처 데이터셋
uspto-grants-2014_09
특허 번호
US08828987B2

연결된 노트

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