Guanidine Sulfate (1:1) → HCID 10225782、化合物

HRID 861124

反応式

HRID 861124 の反応式
[Br:1][C:2]1[CH:3]=[C:4]([C:8]2[C:22]([C:23](=O)/[CH:24]=[CH:25]/N(C)C)=[C:11]3[CH:12]=[CH:13][CH:14]=[C:15]([NH:16][CH:17]4[CH2:21][CH2:20][CH2:19][CH2:18]4)[N:10]3[N:9]=2)[CH:5]=[CH:6][CH:7]=1.S(O)(O)(=O)=O.[NH2:35][C:36]([NH2:38])=[NH:37]>>[NH2:37][C:36]1[N:38]=[C:23]([C:22]2[C:8]([C:4]3[CH:5]=[CH:6][CH:7]=[C:2]([Br:1])[CH:3]=3)=[N:9][N:10]3[C:15]([NH:16][CH:17]4[CH2:18][CH2:19][CH2:20][CH2:21]4)=[CH:14][CH:13]=[CH:12][C:11]=23)[CH:24]=[CH:25][N:35]=1

参加物

3

反応物 2

HCID 499987Guanidine Sulfate (1:1)HCID 57463868HCID 57463868、化合物

生成物 1

HCID 10225782HCID 10225782、化合物収率 77%

実験手順

In a similar manner as described in Example 1 from (2E)-1-[2-(3-bromophenyl)-7-(cyclopentylamino)pyrazolo[1,5-a]pyridin-3-yl]-3-(dimethylamino)-2-propen-1-one (500 mg, 1.1 mmol) and guanidine sulfate (358 mg, 1.65 mmol), N-[3-(2-amino-4-pyrimidinyl)-2-(3-bromophenyl)pyrazolo[1,5-a]pyridin-7-yl]-N-cyclopentylamine (380 mg, 77%) was obtained as a yellow solid. 1H NMR (CDCl3): δ 8.01 (d, 1H), 7.84 (s, 1H), 7.64 (d, 1H), 7.54–7.49 (m, 2H), 7.30–7.22 (m, 2H), 6.36 (d, 1H), 6.01 (d, 1H), 5.97 (d, 1H), 4.95 (broad s, 2H), 3.97 (m, 1H), 2.12 (m, 2H), 1.79–1.57 (m, 6H); MS m/z 448 (M+1); Anal. Calcd. for C22H21N6Br: C, 58.80; H, 4.71; N,18.70. Found: C, 58.61; H, 4.75; N, 18.58.

出典と根拠

ORDレコード
ord-699b3813e1504c149c95c2be307a9f61
出典データセット
uspto-grants-2006_12
特許番号
US07153855B2

関連ノート

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