2-Aminothiazole → (RS)-N-(ethoxycarbonyl)-S-methyl-S-[3-({[4-(thiazol-2-ylamino)quinazolin-7-yl]amino}methyl)phenyl]sulphoximide

HRID 249958노트

반응식

HRID 249958 반응식
C([C:3]1[CH:8]=[CH:7][C:6]([NH:9][CH2:10][C:11]2[CH:16]=[CH:15][CH:14]=[C:13]([S:17]([CH3:25])(=[N:19][C:20]([O:22][CH2:23][CH3:24])=[O:21])=[O:18])[CH:12]=2)=[CH:5][C:4]=1[N:26]=[CH:27][N:28](C)[CH3:29])#N.[NH2:31][C:32]1[S:33][CH:34]=[CH:35][N:36]=1.ClCCl.CO>CO>[CH2:23]([O:22][C:20]([N:19]=[S:17]([CH3:25])([C:13]1[CH:14]=[CH:15][CH:16]=[C:11]([CH2:10][NH:9][C:6]2[CH:5]=[C:4]3[C:3]([C:29]([NH:31][C:32]4[S:33][CH:34]=[CH:35][N:36]=4)=[N:28][CH:27]=[N:26]3)=[CH:8][CH:7]=2)[CH:12]=1)=[O:18])=[O:21])[CH3:24]

참가 물질

5

반응물 3

HCID 21552-AminothiazoleHCID 21226129Dichloromethane methanolHCID 57788040N'-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzylamino}phenyl)-N,N-dimethylformimidamide

생성물 1

HCID 44197696(RS)-N-(ethoxycarbonyl)-S-methyl-S-[3-({[4-(thiazol-2-ylamino)quinazolin-7-yl]amino}methyl)phenyl]sulphoximide수율 43%

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]benzylamino}phenyl)-N,N-dimethylformimidamide (90 mg, 0.21 mmol) with 2-aminothiazole (26 mg, 0.25 mmol) and chromatographic purification (silica gel, dichloromethane/methanol: 0→30% methanol) gives the desired product in 43% yield (43 mg).

출처 및 근거

ORD 기록
ord-621789a39ea5407cb0fccd0f799aaa4a
출처 데이터셋
uspto-grants-2011_01
특허 번호
US07863283B2

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