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

HRID 1037691ノート

反応式

HRID 1037691 の反応式
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

参加物

6

反応物 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

生成物 1

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

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒

実験手順

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.

後処理

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

出典と根拠

ORDレコード
ord-cf1e41f6ebec40d1885000ee06dcd2f2
出典データセット
uspto-grants-2013_10
特許番号
US08546565B2

反応ノート

読み込み中…