Z-O-tert-butyl-L-serine N-hydroxysuccinimide ester → HCID 178423965、化合物

HRID 874876

反応式

HRID 874876 の反応式
CC1C=CC=C2C=1C(=O)N(C1C=CC=CC=1)C(C(NC1N=CN=C3C=1N=CN3)CC)=N2.O=C1CCC(=O)N1OC(=O)C(NC(OCC1C=CC=CC=1)=O)COC(C)(C)C.O=C1CCC(=O)N1OC(=O)C(NC(OCC1C=CC=CC=1)=O)CC.[NH2:84][C:85]1[N:93]=[C:92]2[C:88]([NH:89][CH:90]=[N:91]2)=[C:87](Br)[N:86]=1.BrC1N=CN=C2C=1NC=N2.NC1N=C2C(N=CN2)=C([NH:115][CH:116]([C:123]2[N:132]([C:133]3[CH:138]=[CH:137][CH:136]=[CH:135][CH:134]=3)[C:131](=[O:139])[C:130]3[C:125](=[CH:126][CH:127]=[CH:128][C:129]=3[CH3:140])[N:124]=2)[CH2:117][O:118]C(C)(C)C)N=1>FC(F)(F)C(O)=O>[NH2:84][C:85]1[N:93]=[C:92]2[C:88]([N:89]=[CH:90][NH:91]2)=[C:87]([NH:115][CH:116]([C:123]2[N:132]([C:133]3[CH:134]=[CH:135][CH:136]=[CH:137][CH:138]=3)[C:131](=[O:139])[C:130]3[C:125](=[CH:126][CH:127]=[CH:128][C:129]=3[CH3:140])[N:124]=2)[CH2:117][OH:118])[N:86]=1

参加物

8

反応物 6

HCID 2729196Z-O-tert-butyl-L-serine N-hydroxysuccinimide esterHCID 5287830Purine, 6-bromo-HCID 61011392-Amino-6-bromopurineHCID 12961228(2,5-Dioxopyrrolidin-1-yl) 2-(phenylmethoxycarbonylamino)butanoateHCID 178423963HCID 178423963、化合物HCID 178456854HCID 178456854、化合物

生成物 1

HCID 178423965HCID 178423965、化合物

試薬・触媒・溶媒 1

HCID 6422Trifluoroacetic acid溶媒

実験手順

Compound 68 was prepared using the general procedure described above with respect to compound 14, but 2-benzyloxycarbonylamino-3-tert-butoxy-propionic acid 2,5-dioxo-pyrrolidin-1-yl ester was substituted for 2-benzyloxycarbonylaminobutyric acid 2,5-dioxo-pyrrolidin-1-yl ester in step B, and 2-amino-6-bromopurine was substituted for 6-bromopurine in step D. The obtained 2-[1-(2-amino-9H-purin-6-ylamino) -2-tert-butoxy-ethyl]-5-methyl-3-phenyl-3H-quinazolin-4-one was then dissolved in trifluoroacetic acid and allowed to stir at ambient temperature for 5 hours. Purification by LC provided the product 68 as a white solid. MS (ES): m/z 429 (M+H), 215, 206, 151. Compound 68 is shown below.

後処理

  1. customCompound 68 was prepared
  2. customPurification by LC

出典と根拠

ORDレコード
ord-01a2d5fea9a84168898b2660165e6542
出典データセット
uspto-grants-2015_03
特許番号
US08980901B2

関連ノート

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