Pyridine → N-[(3-{4-[(Acetylamino)methyl]phenyl}-2-oxo-1,3-oxazolidin-5-yl)methyl]-5-chloro-2-thiophenecarboxamide

HRID 41086

반응식

HRID 41086 반응식
[NH2:1][CH2:2][C:3]1[CH:8]=[CH:7][C:6]([N:9]2[CH2:13][CH:12]([CH2:14][NH:15][C:16]([C:18]3[S:19][C:20]([Cl:23])=[CH:21][CH:22]=3)=[O:17])[O:11][C:10]2=[O:24])=[CH:5][CH:4]=1.N1C=CC=CC=1.[C:31](OC(=O)C)(=[O:33])[CH3:32].CCOCC>C1COCC1.ClCCl>[C:31]([NH:1][CH2:2][C:3]1[CH:8]=[CH:7][C:6]([N:9]2[CH2:13][CH:12]([CH2:14][NH:15][C:16]([C:18]3[S:19][C:20]([Cl:23])=[CH:21][CH:22]=3)=[O:17])[O:11][C:10]2=[O:24])=[CH:5][CH:4]=1)(=[O:33])[CH3:32]

참가 물질

7

반응물 4

HCID 1049PyridineHCID 3283Diethyl EtherHCID 7918Acetic AnhydrideHCID 21070786N-({3-[4-(aminomethyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)-5-chloro-2-thiophenecarboxamide

생성물 1

HCID 21070779N-[(3-{4-[(Acetylamino)methyl]phenyl}-2-oxo-1,3-oxazolidin-5-yl)methyl]-5-chloro-2-thiophenecarboxamide

시약·촉매·용매 2

HCID 6344Dichloromethane용매HCID 8028Tetrahydrofuran용매

실험 절차

At 0° C., a mixture of 30 mg (0.082 mmol) of N-({3-[4-(aminomethyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)-5-chloro-2-thiophene-carboxamide (from Example 148) in 1.5 ml of absolute THF and 1.0 ml of absolute dichloromethane, and 0.02 ml of absolute pyridine is mixed with acetic anhydride (0.015 ml, 0.164 mmol). The mixture is stirred at room temperature overnight. Addition of ether and crystallization affords the product. Yield: 30 mg (87% of theory),

후처리

  1. customaffords the product

출처 및 근거

ORD 기록
ord-724e934a70aa45599ac0737d7883d5bf
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08530505B2

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