tert-Butyl 4-(5-aminopyridin-2-yl)piperidine-1-carboxylate → (1',2',3',4',5',6'-Hexahydro-[2,4']bipyridinyl-5-yl)-[7-(3-methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-amine

反応式

C(OC([N:8]1[CH2:13][CH2:12][CH:11]([C:14]2[CH:19]=[CH:18][C:17]([NH2:20])=[CH:16][N:15]=2)[CH2:10][CH2:9]1)=O)(C)(C)C.[CH3:21][S:22]([C:25]1[CH:26]=[C:27]([C:31]2[N:39]3[C:34]([CH:35]=[N:36][C:37](O)=[N:38]3)=[CH:33][CH:32]=2)[CH:28]=[CH:29][CH:30]=1)(=[O:24])=[O:23]>>[N:15]1[CH:16]=[C:17]([NH:20][C:37]2[N:36]=[CH:35][C:34]3=[CH:33][CH:32]=[C:31]([C:27]4[CH:28]=[CH:29][CH:30]=[C:25]([S:22]([CH3:21])(=[O:24])=[O:23])[CH:26]=4)[N:39]3[N:38]=2)[CH:18]=[CH:19][C:14]=1[CH:11]1[CH2:10][CH2:9][NH:8][CH2:13][CH2:12]1

参加物

反応物 2

HCID 59128562tert-Butyl 4-(5-aminopyridin-2-yl)piperidine-1-carboxylate

HCID 178504720HCID 178504720、化合物

生成物 1

HCID 66712069(1',2',3',4',5',6'-Hexahydro-[2,4']bipyridinyl-5-yl)-[7-(3-methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-amine

実験手順

This example was prepared by using 5-Amino-3′,4′,5′,6′-tetrahydro-2′H-[2,4]bipyridinyl-1′-carboxylic acid tert-butyl ester (WO2006/047277) and 7-(3-Methanesulfonyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ol as described in Example 1255c followed by deprotection as described in Example 1223. 1H-NMR (DMSO) δ 9.9 (s, 1H), 9.1 (s, 1H), 8.8 (s, 1H), 8.7 (s, 1H), 8.6 (brs, 1H), 8.4 (d, J=7.9 Hz, 2H), 8.2 (d, J=8.9 Hz, 1H), 8 (d, J=7.9 Hz, 1H), 7.8 (t, 1H), 7.3 (m, 2H), 7 (d, J=4.4 Hz, 1H), 3.4 (m, 2H), 3.36 (s, 3H), 3.0 (m, 3H), 2.0 (m, 2H), 1.85 (m, 2H); LC/MS (ESI+): 449 (M+H).

出典と根拠

ORDレコード: ord-e6d53e10e6034d7f833b40a27a5b2d8b
出典データセット: uspto-grants-2013_06
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08471005B2

反応ノート

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