Hydrochloric Acid → 2-[2-amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]-N-(2-methylaminoethyl)benzenesulfonamide

HRID 1037691노트

반응식

HRID 1037691 반응식
NC1N=C(C(N2CC3C(=CC=CC=3)C2)=O)C2C(=CC=C(C3C=CC=CC=3S(Cl)(=O)=O)C=2)N=1.NCCN(C)C(=O)OC(C)(C)C.[NH2:45][C:46]1[N:55]=[C:54]([C:56]([N:58]2[CH2:66][C:65]3[C:60](=[CH:61][CH:62]=[CH:63][CH:64]=3)[CH2:59]2)=[O:57])[C:53]2[C:48](=[CH:49][CH:50]=[C:51]([C:67]3[CH:72]=[CH:71][CH:70]=[CH:69][C:68]=3[S:73]([NH:76][CH2:77][CH2:78][N:79](C)[C:80](=O)OC(C)(C)C)(=[O:75])=[O:74])[CH:52]=2)[N:47]=1.Cl>O1CCOCC1>[NH2:45][C:46]1[N:55]=[C:54]([C:56]([N:58]2[CH2:66][C:65]3[C:60](=[CH:61][CH:62]=[CH:63][CH:64]=3)[CH2:59]2)=[O:57])[C:53]2[C:48](=[CH:49][CH:50]=[C:51]([C:67]3[CH:72]=[CH:71][CH:70]=[CH:69][C:68]=3[S:73]([NH:76][CH2:77][CH2:78][NH:79][CH3:80])(=[O:74])=[O:75])[CH:52]=2)[N:47]=1

참가 물질

6

반응물 4

HCID 313Hydrochloric AcidHCID 2756424N-Boc-N-methylethylenediamineHCID 584571942-[2-Amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]benzenesulfonyl chlorideHCID 67433857Tert-butyl (2-{2-[2-amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]benzenesulfonylamino}ethyl)methylcarbamate

생성물 1

HCID 467019522-[2-amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]-N-(2-methylaminoethyl)benzenesulfonamide

시약·촉매·용매 1

HCID 312751,4-Dioxane용매

실험 절차

The product is obtained analogously to the preparation of “A64” by reaction of 2-[2-amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]benzenesulfonyl chloride and tert-butyl (2-aminoethyl)methylcarbamate. The resultant tert-butyl (2-{2-[2-amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]benzenesulfonylamino}ethyl)methylcarbamate is treated directly with 1 M HCl in dioxane, causing the protecting group to be cleaved. The purification is carried out by means of preparative column chromatography.

후처리

  1. customThe product is obtained analogously to the preparation of “A64”
  2. customThe purification

출처 및 근거

ORD 기록
ord-cf1e41f6ebec40d1885000ee06dcd2f2
출처 데이터셋
uspto-grants-2013_10
특허 번호
US08546565B2

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