Hexane → (RS)-S-[3-({[4-(Cyclobutylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)phenyl]-N-(ethoxycarbonyl)-S-methylsulphoximide

HRID 249938

반응식

HRID 249938 반응식
C([C:3]1[CH:8]=[C:7]([O:9][CH3:10])[C:6]([O:11][CH2:12][C:13]2[CH:18]=[CH:17][CH:16]=[C:15]([S:19]([CH3:27])(=[N:21][C:22]([O:24][CH2:25][CH3:26])=[O:23])=[O:20])[CH:14]=2)=[CH:5][C:4]=1[N:28]=[CH:29][N:30](C)[CH3:31])#N.[CH:33]1([NH2:37])[CH2:36][CH2:35][CH2:34]1.CCCCCC.ClCCl.CO>CO>[CH:33]1([NH:37][C:31]2[C:3]3[C:4](=[CH:5][C:6]([O:11][CH2:12][C:13]4[CH:14]=[C:15]([S:19]([CH3:27])(=[N:21][C:22]([O:24][CH2:25][CH3:26])=[O:23])=[O:20])[CH:16]=[CH:17][CH:18]=4)=[C:7]([O:9][CH3:10])[CH:8]=3)[N:28]=[CH:29][N:30]=2)[CH2:36][CH2:35][CH2:34]1

참가 물질

6

반응물 4

HCID 8058HexaneHCID 75645CyclobutylamineHCID 21226129Dichloromethane methanolHCID 57788001N'-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide

생성물 1

HCID 57788036(RS)-S-[3-({[4-(Cyclobutylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)phenyl]-N-(ethoxycarbonyl)-S-methylsulphoximide수율 74%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

According to GWP 5, the reaction of N′-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide (72 mg, 0.16 mmol) with cyclobutylamine (16 μL, 0.19 mmol) and chromatographic purification (silica gel, amino column, hexane, dichloromethane/methanol: 0→5% methanol) gives the desired product in 74% yield (56 mg).

출처 및 근거

ORD 기록
ord-d7cc002d82424ac98a57459d0b68d588
출처 데이터셋
uspto-grants-2011_01
특허 번호
US07863283B2

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