Trifluoroacetic acid → (E)-4-(8-Morpholino-2-(2-(quinolin-2-yl)vinyl)imidazo[1,2-a]pyrazin-5-yl)benzoic acid trifluoroacetic acid salt

HRID 1772701

反応式

HRID 1772701 の反応式
Br[C:2]1[N:7]2[CH:8]=[C:9](/[CH:11]=[CH:12]/[C:13]3[CH:22]=[CH:21][C:20]4[C:15](=[CH:16][CH:17]=[CH:18][CH:19]=4)[N:14]=3)[N:10]=[C:6]2[C:5]([N:23]2[CH2:28][CH2:27][O:26][CH2:25][CH2:24]2)=[N:4][CH:3]=1.C([O:33][C:34]([C:36]1[CH:41]=[CH:40][C:39](B2OC(C)(C)C(C)(C)O2)=[CH:38][CH:37]=1)=[O:35])(C)(C)C.[C:51]([OH:57])([C:53]([F:56])([F:55])[F:54])=[O:52]>>[F:54][C:53]([F:56])([F:55])[C:51]([OH:57])=[O:52].[O:26]1[CH2:27][CH2:28][N:23]([C:5]2[C:6]3[N:7]([CH:8]=[C:9](/[CH:11]=[CH:12]/[C:13]4[CH:22]=[CH:21][C:20]5[C:15](=[CH:16][CH:17]=[CH:18][CH:19]=5)[N:14]=4)[N:10]=3)[C:2]([C:39]3[CH:40]=[CH:41][C:36]([C:34]([OH:35])=[O:33])=[CH:37][CH:38]=3)=[CH:3][N:4]=2)[CH2:24][CH2:25]1

参加物

4

反応物 3

HCID 6422Trifluoroacetic acidHCID 43767661,1-Dimethylethyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoateHCID 117728505(E)-4-(5-Bromo-2-(2-(quinolin-2-yl)vinyl)imidazo[1,2-a]pyrazin-8-yl)morpholine

生成物 1

HCID 117728004(E)-4-(8-Morpholino-2-(2-(quinolin-2-yl)vinyl)imidazo[1,2-a]pyrazin-5-yl)benzoic acid trifluoroacetic acid salt

実験手順

The title compound was prepared from compound 2b and 4-(tert-butoxycarbonyl)phenylboronic acid pinacol ester using the methods described in Example 1, Step G, followed by the deprotection of the resulting product with TFA using the methods described in Example 6, Step B. Mass Spectrum (LCMS, ESI pos.) Calcd. for C28H23N5O3: 478.2 [M+H]. found 478.1.

出典と根拠

ORDレコード
ord-427ad22895d04c22b48460bfdb3fb69c
出典データセット
uspto-grants-2016_02
特許番号
US09249163B2

関連ノート

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