Oxalyl chloride → HCID 57749200、化合物

HRID 1874406

反応式

HRID 1874406 の反応式
CN1C(C(NC2C=CC=C(OC3C=CC4N(C=C(NC(=O)C(F)(F)F)N=4)C=3)C=2)=O)=CC(C)=N1.[CH3:34][N:35]1[N:39]=[N:38][C:37]([C:40]([OH:42])=O)=[N:36]1.C(Cl)(=O)C(Cl)=O.[NH2:49][C:50]1[CH:51]=[C:52]([CH:69]=[CH:70][CH:71]=1)[O:53][C:54]1[CH:55]=[CH:56][C:57]2[N:58]([CH:60]=[C:61]([NH:63][C:64]([CH:66]3[CH2:68][CH2:67]3)=[O:65])[N:62]=2)[CH:59]=1>CN(C)C=O.CN(C)C(=O)C.O1CCCC1>[CH:66]1([C:64]([NH:63][C:61]2[N:62]=[C:57]3[CH:56]=[CH:55][C:54]([O:53][C:52]4[CH:51]=[C:50]([NH:49][C:40]([C:37]5[N:38]=[N:39][N:35]([CH3:34])[N:36]=5)=[O:42])[CH:71]=[CH:70][CH:69]=4)=[CH:59][N:58]3[CH:60]=2)=[O:65])[CH2:67][CH2:68]1

参加物

8

反応物 4

HCID 65578Oxalyl chlorideHCID 3231942-methyl-2H-1,2,3,4-tetrazole-5-carboxylic acidHCID 577492691,3-dimethyl-N-[3-({2-[(trifluoroacetyl)amino]imidazo[1,2-a]pyridin-6-yl}oxy)phenyl]-1H-pyrazole-5-carboxamideHCID 57749361N-[6-(3-aminophenoxy)imidazo[1,2-a]pyridin-2-yl]cyclopropanecarboxamide

生成物 1

HCID 57749200HCID 57749200、化合物収率 54.2%

試薬・触媒・溶媒 3

HCID 6228Dimethylformamide触媒HCID 8028Tetrahydrofuran溶媒HCID 31374Dimethylacetamide溶媒

実験手順

In the same manner as in Example 7-4 and using a mixture of 1-methyl-1H-tetrazole-5-carboxylic acid (1) and 2-methyl-2H-tetrazole-5-carboxylic acid (2) ((1):(2)≈1:1, 200 mg, 1.56 mmol), oxalyl chloride (141 μL, 1.72 mmol), N-[6-(3-aminophenoxy)imidazo[1,2-a]pyridin-2-yl]cyclopropanecarboxamide (70.0 mg, 0.227 mmol), tetrahydrofuran (10 mL), N,N-dimethylformamide (1 drop) and N,N-dimethylacetamide (3 mL) as starting materials, the title compound (51.5 mg, 54%) was obtained as a white solid.

出典と根拠

ORDレコード
ord-4578945f6fe04e568cee5385ec49218b
出典データセット
uspto-grants-2012_11
特許番号
US08304557B2

関連ノート

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